Page last updated: 2024-11-12
glanatec
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Cross-References
ID Source | ID |
---|---|
PubMed CID | 11625386 |
CHEMBL ID | 4594454 |
MeSH ID | M000608669 |
Synonyms (45)
Synonym |
---|
K115 , |
k-115 |
ripasudil hydrochloride hydrate (jan) |
glanatec (tn) |
D10463 |
glanatec |
ripasudil hydrochloride dihydrate |
isoquinoline, 4-fluoro-5-(((2s)-hexahydro-2-methyl-1h-1,4-diazepin-1-yl)sulfonyl)-, hydrochloride, hydrate (1:1:2) |
ripasudil hydrochloride hydrate |
ripasudil hydrochloride hydrate [jan] |
ripasudil hydrochloride dihydrate [mi] |
887375-67-9 |
k-115-r |
ripasudil hydrochloride dihydrate [who-dd] |
016TTR32QF , |
1h-1,4-diazepine, 1-((4-fluoro-5-isoquinolinyl)sulfonyl)hexahydro-2-methyl-, monohydrochloride, dihydrate, (2s)- |
S7995 |
unii-016ttr32qf |
CS-3401 |
AC-30884 |
HY-15685 |
k-115 hydrochloride dihydrate |
4-fluoro-5-[[(2s)-2-methyl-1,4-diazepan-1-yl]sulfonyl]isoquinoline;dihydrate;hydrochloride |
AKOS027338678 |
4-fluoro-5-{[(2s)-2-methyl-1,4-diazepan-1-yl]sulfonyl}isoquinoline dihydrate hydrochloride |
mfcd26960897 |
(s)-4-fluoro-5-((2-methyl-1,4-diazepan-1-yl)sulfonyl)isoquinoline hydrochloride dihydrate |
4-fluoro-5-[(2s)-2-methyl-1,4-diazepane-1-sulfonyl]isoquinoline dihydrate hydrochloride |
ripasudil(k-115) |
ripasudil (k-115) dihydrate |
ripasudil hcl dihydrate |
887375-67-9 (hcl dihydrate) |
ripasudil (k-115) hydrochloride di |
ripasudil (k-115) |
BCP11082 |
AMY23739 |
EX-A3346 |
CCG-268603 |
ripasudil monohydrochloride dihydrate |
Q27231405 |
AS-55803 |
k-115k-115 |
CHEMBL4594454 |
(2s)-1-[(4-fluoro-5-isoquinolinyl)sulfonyl]hexahydro-2-methyl-1h-1,4-diazepine monohydrochloride dihydrate;k-115 hydrochloride dihydrate |
A900057 |
Research Excerpts
Toxicity
Compound-Compound Interactions
Excerpt | Reference | Relevance |
---|---|---|
" However, no studies have evaluated ripasudil combined with β-blockers and prostaglandin analogues." | ( Additive Intraocular Pressure-Lowering Effects of the Rho Kinase Inhibitor Ripasudil (K-115) Combined With Timolol or Latanoprost: A Report of 2 Randomized Clinical Trials. Abe, H; Araie, M; Inoue, T; Kuwayama, Y; Suganami, H; Tanihara, H; Yamamoto, T, 2015) | 0.42 |
"These clinical trials found additive IOP-lowering effects of ripasudil from placebo at trough and peak levels in combination with timolol and at peak level in combination with latanoprost." | ( Additive Intraocular Pressure-Lowering Effects of the Rho Kinase Inhibitor Ripasudil (K-115) Combined With Timolol or Latanoprost: A Report of 2 Randomized Clinical Trials. Abe, H; Araie, M; Inoue, T; Kuwayama, Y; Suganami, H; Tanihara, H; Yamamoto, T, 2015) | 0.42 |
Dosage Studied
Excerpt | Relevance | Reference |
---|---|---|
"02% dosed QD (p." | ( Phase 3 Clinical Trial Comparing the Safety and Efficacy of Netarsudil to Ripasudil in Patients with Primary Open-Angle Glaucoma or Ocular Hypertension: Japan Rho Kinase Elevated Intraocular Pressure Treatment Trial (J-ROCKET). Araie, M; Aso, K; Hollander, DA; Iwata, R; Kanemoto, K; Kopczynski, CC; Senchyna, M; Sugiyama, K, 2023) | 0.91 |
"This study investigated the effects of dexamethasone (Dex) on human trabecular meshwork (TM) cells, a model of glucocorticoid-induced glaucoma, and evaluated the impact of ripasudil (Rip) as a co-delivery or sequential dosing strategy." | ( The Effects of ROCK Inhibitor on Prevention of Dexamethasone-Induced Glaucoma Phenotype in Human Trabecular Meshwork Cells. Debele, TA; Kao, WW; Mount, ZF; Park, YC; Yuan, Y, 2023) | 0.91 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (2)
Inhibition Measurements
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Rho-associated protein kinase 2 | Homo sapiens (human) | IC50 (µMol) | 0.0214 | 0.0002 | 0.5780 | 10.0000 | AID1887129 |
Rho-associated protein kinase 1 | Homo sapiens (human) | IC50 (µMol) | 0.0640 | 0.0004 | 0.8549 | 10.0000 | AID1887128 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Biological Processes (86)
Molecular Functions (14)
Ceullar Components (16)
Bioassays (15)
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1887147 | Antiglaucoma activity in microspheres induced chronic ocular hypertension C57BL/6J mouse model assessed as reduction in intraocular pressure at 0.2% solution administered via topical instillation for three times per day and measured at 1 to 6 hrs post ins | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities. |
AID1887160 | Antiglaucoma activity in microspheres induced chronic ocular hypertension C57BL/6J mouse model assessed as reduction in intraocular pressure at 0.2% solution administered via topical instillation for three times per day and measured at 4 hrs post instilla | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities. |
AID1887130 | Downregulation of phosphorylated MLC expression in HTM cells at 10 uM incubated for 1 hr by Western blotting analysis | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities. |
AID1887131 | Downregulation of MLC expression in HTM cells at 10 uM incubated for 1 hr by Western blotting analysis | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities. |
AID1887129 | Inhibition of ROCK2 (unknown origin) using biotin as substrate incubated for 1 hr by HTRF assay | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities. |
AID1887141 | Inhibtion of mitochondrial respiration in HTM cells assessed as oxygen consumption rate by measuring decrease in coupling efficiency at 10 uM incubated for 1 hr by Seahorse XF24 extracellular flux analyzer | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities. |
AID1887159 | Antiglaucoma activity in microspheres induced chronic ocular hypertension C57BL/6J mouse model assessed as reduction in intraocular pressure at 0.2% solution administered via topical instillation for three times per day and measured at 1 hr post instillat | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities. |
AID1887138 | Inhibtion of mitochondrial respiration in HTM cells assessed as oxygen consumption rate by measuring decrease in basal respiration at 10 uM incubated for 1 hr by Seahorse XF24 extracellular flux analyzer | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities. |
AID1887139 | Inhibtion of mitochondrial respiration in HTM cells assessed as oxygen consumption rate by measuring decrease in ATP production at 10 uM incubated for 1 hr by Seahorse XF24 extracellular flux analyzer | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities. |
AID1887128 | Inhibition of ROCK1 (unknown origin) using biotin as substrate incubated for 1 hr by HTRF assay | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities. |
AID1887132 | Effect on MLC expression in HTM cells assessed as reduction in phosphorylated MLC/MLC ratio at 10 uM incubated for 1 hr by densitometry analysis | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities. |
AID1887136 | Induction of reversible F-actin depolymerization in HTM cells assessed as irregular arrangement of fiber bundles at 10 uM incubated for 1 hr and further incubated for 4 hrs in drug free medium by rhodamine phalloidin staining based confocal scanning micro | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities. |
AID1887142 | Inhibtion of mitochondrial respiration in HTM cells assessed as oxygen consumption rate by measuring decrease in proton leak at 10 uM incubated for 1 hr by Seahorse XF24 extracellular flux analyzer | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities. |
AID1887152 | Ocular toxicity in C57BL/6J mouse assessed as effect on conjunctival hyperemia at 0.2% solution administered via topical instillation and measured at 1 to 4 hrs post instillation | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities. |
AID1887140 | Inhibtion of mitochondrial respiration in HTM cells assessed as oxygen consumption rate by measuring decrease in maximal respiration at 10 uM incubated for 1 hr by Seahorse XF24 extracellular flux analyzer | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (104)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 54 (51.92) | 24.3611 |
2020's | 50 (48.08) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Market Indicators
Research Demand Index: 43.71
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.
| This Compound (43.71) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 12 (11.32%) | 5.53% |
Reviews | 10 (9.43%) | 6.00% |
Case Studies | 5 (4.72%) | 4.05% |
Observational | 5 (4.72%) | 0.25% |
Other | 74 (69.81%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |