Page last updated: 2024-10-15

nn 414

Description

NN 414: a hypoglycemic agent with insulin release modulating and potassium channel activating activities; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID135410911
CHEMBL ID135191
SCHEMBL ID2109690
MeSH IDM0451742

Synonyms (38)

Synonym
2h-thieno(3,2-e)-1,2,4-thiadiazin-3-amine, 6-chloro-n-(1-methylcyclopropyl)-, 1,1-dioxide
6-chloro-3-((1-methylcyclopropyl)amino)-4h-thieno(3,2-e)-1,2,4-thiadiazine 1,1-dioxide
y79681glmg ,
tifenazoxide [inn]
unii-y79681glmg
nn414
6-chloro-n-(1-methylcyclopropyl)-1,1-dioxo-1,4-dihydro-1lambda(sup 6)-thieno(3,2-e)(1,2,4)thiadiazin-3-amine
nn-414
tifenazoxide
CHEMBL135191 ,
bdbm50118359
6-chloro-3-(1-methylcyclopropyl)-amino-4h-thieno[3,2-e]-1,2,4-thiadiazine1,1-dioxide
(2-chloro-7,7-dioxo-4,7-dihydro-1,7lambda*6*-dithia-4,6-diaza-inden-5-yl)-(1-methyl-cyclopropyl)-amine
(2-chloro-7,7-dioxo-4,7-dihydro-1,7-dithia-4,6-diaza-inden-5-yl)-(1-methyl-cyclopropyl)-amine
nn 414
279215-43-9
6-chloro-n-(1-methylcyclopropyl)-1,1-dioxo-4h-thieno[3,2-e][1,2,4]thiadiazin-3-amine
6-chloro-3-(1-methyl-cyclopropyl)amino-4h-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide
6-chloro-3-(1-methylcyclopropyl)amino-4h-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide
KYSFUHHFTIGRJN-UHFFFAOYSA-N
smr004701658
MLS006010676
SCHEMBL2109690
6-chloro-3-(1-methylcyclopropylamino)-4h-thieno[3,2-e][1,2,4]thiadiazine-1,1-dioxide
sr-01000945038
SR-01000945038-1
nn414, >=98% (hplc)
HY-119322
CS-0067041
6-chloro-n-(1-methylcyclopropyl)-1,1-dioxo-4h-thieno[3,2-e][1,2,4]thiadiazin-3-imine
Q27294341
MS-24167
6-chloro-3-((1-methylcyclopropyl)amino)-2h-thieno[3,2-e][1,2,4]thiadiazine 1,1-dioxide ,
8-chloro-n-(1-methylcyclopropyl)-2,2-dioxo-2$l^{6},9-dithia-3,5-diazab icyclo[4.3.0]nona-3,7,10-trien-4-amine
6-chloro-3-[(1-methylcyclopropyl)amino]-1lambda~6~-thieno[3,2-e][1,2,4]thiadiazine-1,1(4h)-dione
DTXSID60870307
E98922
AKOS040742742

Dosage Studied

ExcerptReference
" Two chronic dosing protocols of NN414 of 3 weeks' duration were compared with appropriate vehicle-treated controls."( NN414, a SUR1/Kir6.2-selective potassium channel opener, reduces blood glucose and improves glucose tolerance in the VDF Zucker rat.
Bodvarsdottir, TB; Brand, CL; Carr, RD; Hansen, JB; Sturis, J, 2003
)
" The study consisted of a baseline day and a dosing day."( The effects of NN414, a SUR1/Kir6.2 selective potassium channel opener, in healthy male subjects.
Dyrberg, T; Kecskes, A; Kruse, M; Møss, J; Rost, KL; Zdravkovic, M, 2005
)
"In vivo dose-response studies with NN414 delivered intravenously to normal Sprague-Dawley rats before the induction of controlled hypoglycemia were performed."( Amplified hormonal counterregulatory responses to hypoglycemia in rats after systemic delivery of a SUR-1-selective K(+) channel opener?
Cheng, H; Ding, Y; Fan, X; Gram, DX; McCrimmon, RJ; Sherwin, RS, 2008
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Coagulation factor VIIHomo sapiens (human)IC50 (µMol)696.00000.00020.83363.3000AID267952
Tissue factorHomo sapiens (human)IC50 (µMol)696.00000.00010.734410.0000AID267952
ATP-binding cassette sub-family C member 8Homo sapiens (human)IC50 (µMol)309.32120.00431.07038.2000AID208994; AID208995; AID208996; AID267952; AID267953
ATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)IC50 (µMol)309.32120.00431.36868.2000AID208994; AID208995; AID208996; AID267952; AID267953
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 8Homo sapiens (human)EC50 (µMol)0.27670.02191.12578.8000AID267948; AID286541; AID286542
ATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)EC50 (µMol)0.27670.02190.97088.8000AID267948; AID286541; AID286542
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (78)

Processvia Protein(s)Taxonomy
response to hypoxiaCoagulation factor VIIHomo sapiens (human)
positive regulation of leukocyte chemotaxisCoagulation factor VIIHomo sapiens (human)
blood coagulationCoagulation factor VIIHomo sapiens (human)
circadian rhythmCoagulation factor VIIHomo sapiens (human)
response to carbon dioxideCoagulation factor VIIHomo sapiens (human)
positive regulation of platelet-derived growth factor receptor signaling pathwayCoagulation factor VIIHomo sapiens (human)
protein processingCoagulation factor VIIHomo sapiens (human)
positive regulation of blood coagulationCoagulation factor VIIHomo sapiens (human)
positive regulation of cell migrationCoagulation factor VIIHomo sapiens (human)
animal organ regenerationCoagulation factor VIIHomo sapiens (human)
positive regulation of TOR signalingCoagulation factor VIIHomo sapiens (human)
response to estradiolCoagulation factor VIIHomo sapiens (human)
response to vitamin KCoagulation factor VIIHomo sapiens (human)
response to genisteinCoagulation factor VIIHomo sapiens (human)
response to estrogenCoagulation factor VIIHomo sapiens (human)
positive regulation of positive chemotaxisCoagulation factor VIIHomo sapiens (human)
response to growth hormoneCoagulation factor VIIHomo sapiens (human)
response to cholesterolCoagulation factor VIIHomo sapiens (human)
response to thyroxineCoagulation factor VIIHomo sapiens (human)
response to Thyroid stimulating hormoneCoagulation factor VIIHomo sapiens (human)
response to 2,3,7,8-tetrachlorodibenzodioxineCoagulation factor VIIHomo sapiens (human)
response to astaxanthinCoagulation factor VIIHomo sapiens (human)
response to thyrotropin-releasing hormoneCoagulation factor VIIHomo sapiens (human)
positive regulation of gene expressionTissue factorHomo sapiens (human)
positive regulation of interleukin-8 productionTissue factorHomo sapiens (human)
positive regulation of endothelial cell proliferationTissue factorHomo sapiens (human)
activation of plasma proteins involved in acute inflammatory responseTissue factorHomo sapiens (human)
activation of blood coagulation via clotting cascadeTissue factorHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processTissue factorHomo sapiens (human)
blood coagulationTissue factorHomo sapiens (human)
positive regulation of platelet-derived growth factor receptor signaling pathwayTissue factorHomo sapiens (human)
protein processingTissue factorHomo sapiens (human)
positive regulation of cell migrationTissue factorHomo sapiens (human)
positive regulation of TOR signalingTissue factorHomo sapiens (human)
positive regulation of angiogenesisTissue factorHomo sapiens (human)
positive regulation of positive chemotaxisTissue factorHomo sapiens (human)
cytokine-mediated signaling pathwayTissue factorHomo sapiens (human)
intracellular glucose homeostasisATP-binding cassette sub-family C member 8Homo sapiens (human)
potassium ion transportATP-binding cassette sub-family C member 8Homo sapiens (human)
female pregnancyATP-binding cassette sub-family C member 8Homo sapiens (human)
memoryATP-binding cassette sub-family C member 8Homo sapiens (human)
visual learningATP-binding cassette sub-family C member 8Homo sapiens (human)
response to pHATP-binding cassette sub-family C member 8Homo sapiens (human)
response to xenobiotic stimulusATP-binding cassette sub-family C member 8Homo sapiens (human)
response to zinc ionATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of low-density lipoprotein particle clearanceATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of angiogenesisATP-binding cassette sub-family C member 8Homo sapiens (human)
response to lipopolysaccharideATP-binding cassette sub-family C member 8Homo sapiens (human)
positive regulation of tumor necrosis factor productionATP-binding cassette sub-family C member 8Homo sapiens (human)
response to insulinATP-binding cassette sub-family C member 8Homo sapiens (human)
positive regulation of insulin secretion involved in cellular response to glucose stimulusATP-binding cassette sub-family C member 8Homo sapiens (human)
positive regulation of potassium ion transportATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of insulin secretionATP-binding cassette sub-family C member 8Homo sapiens (human)
neuromuscular processATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of glial cell proliferationATP-binding cassette sub-family C member 8Homo sapiens (human)
glutamate secretion, neurotransmissionATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of neuroblast migrationATP-binding cassette sub-family C member 8Homo sapiens (human)
cellular response to organic substanceATP-binding cassette sub-family C member 8Homo sapiens (human)
potassium ion transmembrane transportATP-binding cassette sub-family C member 8Homo sapiens (human)
inorganic cation transmembrane transportATP-binding cassette sub-family C member 8Homo sapiens (human)
positive regulation of uterine smooth muscle relaxationATP-binding cassette sub-family C member 8Homo sapiens (human)
positive regulation of tight junction disassemblyATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of blood-brain barrier permeabilityATP-binding cassette sub-family C member 8Homo sapiens (human)
potassium ion import across plasma membraneATP-binding cassette sub-family C member 8Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 8Homo sapiens (human)
action potentialATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to hypoxiaATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to ischemiaATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ventricular cardiac muscle tissue developmentATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
glucose metabolic processATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
apoptotic processATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
determination of adult lifespanATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to xenobiotic stimulusATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to estradiolATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to ATPATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to testosteroneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
regulation of membrane potentialATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
negative regulation of insulin secretionATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
regulation of insulin secretionATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
nervous system processATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
CAMKK-AMPK signaling cascadeATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cellular response to nicotineATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cellular response to glucose stimulusATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cellular response to tumor necrosis factorATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
potassium ion transmembrane transportATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
inorganic cation transmembrane transportATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
regulation of presynaptic membrane potentialATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
positive regulation of protein localization to plasma membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to resveratrolATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
potassium ion import across plasma membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
regulation of monoatomic ion transmembrane transportATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
serine-type endopeptidase activityCoagulation factor VIIHomo sapiens (human)
signaling receptor bindingCoagulation factor VIIHomo sapiens (human)
calcium ion bindingCoagulation factor VIIHomo sapiens (human)
protein bindingCoagulation factor VIIHomo sapiens (human)
serine-type peptidase activityCoagulation factor VIIHomo sapiens (human)
serine-type endopeptidase activityTissue factorHomo sapiens (human)
protease bindingTissue factorHomo sapiens (human)
protein bindingTissue factorHomo sapiens (human)
phospholipid bindingTissue factorHomo sapiens (human)
cytokine receptor activityTissue factorHomo sapiens (human)
ATP-activated inward rectifier potassium channel activityATP-binding cassette sub-family C member 8Homo sapiens (human)
potassium channel activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 8Homo sapiens (human)
sulfonylurea receptor activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ATP-activated inward rectifier potassium channel activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ATPase-coupled monoatomic cation transmembrane transporter activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ADP bindingATP-binding cassette sub-family C member 8Homo sapiens (human)
transmembrane transporter bindingATP-binding cassette sub-family C member 8Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 8Homo sapiens (human)
voltage-gated potassium channel activityATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
protein bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ATP bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ATP-activated inward rectifier potassium channel activityATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ATPase-coupled monoatomic cation transmembrane transporter activityATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ankyrin bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
potassium ion bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
heat shock protein bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
transmembrane transporter bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
extracellular regionCoagulation factor VIIHomo sapiens (human)
endoplasmic reticulum lumenCoagulation factor VIIHomo sapiens (human)
Golgi lumenCoagulation factor VIIHomo sapiens (human)
plasma membraneCoagulation factor VIIHomo sapiens (human)
vesicleCoagulation factor VIIHomo sapiens (human)
collagen-containing extracellular matrixCoagulation factor VIIHomo sapiens (human)
serine-type peptidase complexCoagulation factor VIIHomo sapiens (human)
extracellular spaceCoagulation factor VIIHomo sapiens (human)
extracellular spaceTissue factorHomo sapiens (human)
plasma membraneTissue factorHomo sapiens (human)
external side of plasma membraneTissue factorHomo sapiens (human)
cell surfaceTissue factorHomo sapiens (human)
membraneTissue factorHomo sapiens (human)
collagen-containing extracellular matrixTissue factorHomo sapiens (human)
serine-type peptidase complexTissue factorHomo sapiens (human)
plasma membraneTissue factorHomo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 8Homo sapiens (human)
inward rectifying potassium channelATP-binding cassette sub-family C member 8Homo sapiens (human)
synaptic vesicle membraneATP-binding cassette sub-family C member 8Homo sapiens (human)
sarcolemmaATP-binding cassette sub-family C member 8Homo sapiens (human)
potassium ion-transporting ATPase complexATP-binding cassette sub-family C member 8Homo sapiens (human)
membraneATP-binding cassette sub-family C member 8Homo sapiens (human)
acrosomal vesicleATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
nuclear envelopeATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
endosomeATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
plasma membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
inward rectifying potassium channelATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
intercalated discATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
T-tubuleATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
axolemmaATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
presynaptic membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
neuronal cell bodyATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cell body fiberATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
glutamatergic synapseATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
plasma membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (37)

Assay IDTitleYearJournalArticle
AID267955Cmax in Sprague-Dawley rat at 1.89 mg/kg, po2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
AID267952Displacement of [3H]glibenclamide from human Kir6.2/SUR1 expressed in HEK293 cells2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
AID267951Reduction in plasma insulin level in po dosed Zucker obese rat after 2 hrs2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
AID267959Half life in Sprague-Dawley rat at 1.89 mg/kg, po2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
AID267944Repolarization of beta-TC3 cells2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
AID248509inhibitory concentration required for repolarization of beta cell membrane potential in presence of 10 mM glucose2004Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
2-(4-Methoxyphenoxy)-5-nitro-N-(4-sulfamoylphenyl)benzamide activates Kir6.2/SUR1 K(ATP) channels.
AID286542Activity at Kir6.2/SUR1 KATP channels expressed in HEK293 cells assessed as activation of K+ currents2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Virtual screening for novel openers of pancreatic K(ATP) channels.
AID267949Inhibition of glucose-stimulated insulin release in Wistar rat islets2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
AID208996Inhibition of [3H]glibenclamide binding to HEK293 cells co-expressing human Sulfonylurea receptor SUR1 and Inward rectifier K+ channel Kir6.2 without ATP2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
AID267947Relaxation of precontracted Wistar rat aorta rings2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
AID267957Oral bioavailability in Sprague-Dawley rat at 1.89 mg/kg, po2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
AID286541Activity at Kir6.2/SUR1 KATP channels expressed in HEK293 cells assessed as repolarization of tolbutamide-induced membrane depolarization2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Virtual screening for novel openers of pancreatic K(ATP) channels.
AID189385Reduction in plasma insulin in 30 min post-injection in rat2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
AID267958Clearance in Sprague-Dawley rat at 1.89 mg/kg, po or 0.89 mg/kg, iv2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
AID172703Maximum change in MAP in rat2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
AID175326Ability to relax phenylephrine-contracted rat aorta rings2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
AID267953Displacement of [3H]glibenclamide from human Kir6.2/SUR1 expressed in HEK293 cells in presence of 2 mM ATP2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
AID188883Maximum reduction in plasma insulin in rat2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
AID248136Concentration required for inhibition of glucose stimulated insulin release from beta TC6 cells2004Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
2-(4-Methoxyphenoxy)-5-nitro-N-(4-sulfamoylphenyl)benzamide activates Kir6.2/SUR1 K(ATP) channels.
AID267946Inhibition of glucose-stimulated insulin release in beta-TC6 cells at 10 uM2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
AID267956Tmax in Sprague-Dawley rat at 1.89 mg/kg, po or 0.89 mg/kg, iv2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
AID267945Inhibition of glucose-stimulated insulin release in betaTC6 cells2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
AID179966Inhibition of glucose-stimulated insulin release from Wistar rat islets2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
AID286543Repolarization of tolbutamide-depolarized beta-TC3 cells2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Virtual screening for novel openers of pancreatic K(ATP) channels.
AID44708Ability to inhibit the release of insulin from the mouse beta-TC6 cell line2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
AID267948Repolarization of HEK293 cells expressing Kir6.2/SUR1 KATP channels2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
AID14000Oral bioavailability in rat (Sprague-Dawley)2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
AID10710Area under the MAP curve measured over 5 min.2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
AID251164Percent efficacy for inhibition of glucose stimulated insulin release from beta TC6 cells2004Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
2-(4-Methoxyphenoxy)-5-nitro-N-(4-sulfamoylphenyl)benzamide activates Kir6.2/SUR1 K(ATP) channels.
AID24886Half life after oral administration to Sprague-Dawley rats2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
AID286544Inhibition of insulin release from rat INS-1E cells2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Virtual screening for novel openers of pancreatic K(ATP) channels.
AID267950Reduction in plasma insulin level in anaesthetized Sprague-Dawley rat at 3 mg/kg, iv2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
AID208994Inhibition of [3H]glibenclamide binding to HEK293 cells co-expressing human Sulfonylurea receptor SUR1 and Inward rectifier K+ channel Kir6.2 at high affinity state with 2 mM MgATP2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
AID176043Vasodilation effects on Wistar rat mesenteric arteries precontracted with phenylephrine2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
AID42092Changes in potassium fluxes assessed in the glucose responsive insulin-producing murine cell line beta-TC32002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
AID208995Inhibition of [3H]glibenclamide binding to HEK293 cells co-expressing human Sulfonylurea receptor SUR1 and Inward rectifier K+ channel Kir6.2 at low affinity state with 2 mM MgATP2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
AID44707Percentage insulin release in vitro in beta-TC6 cells2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's15 (78.95)29.6817
2010's4 (21.05)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (10.00%)5.53%
Reviews1 (5.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other17 (85.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]