TZU 0460: RN given refers to HCl; structure given in first source
ID Source | ID |
---|---|
PubMed CID | 56704 |
CHEMBL ID | 2104871 |
CHEBI ID | 32107 |
SCHEMBL ID | 667643 |
MeSH ID | M0133290 |
Synonym |
---|
MLS002153806 |
altat |
xarcin |
hoe-760 |
roxatidine acetate hydrochloride |
akp-004 |
gastralgin |
tzu-0460 |
tzu 0460 |
2-hydroxy-n-(3-(m-(piperidinomethyl)phenoxy)propyl)acetamide acetate (ester) hydrochloride |
neo h2 |
2-acetoxy-n-(3-(m-(1-piperidinylmethyl)phenoxy)propyl)acetamide hydrochloride |
acetamide, 2-hydroxy-n-(3-(m-(1-piperidinylmethyl)phenoxy)propyl)-, acetate, hydrochloride |
ccris 3347 |
acetamide, 2-(acetyloxy)-n-(3-(3-(1-piperidinylmethyl)phenoxy)propyl-, monohydrochloride |
hoe 760 |
aceroxatidine hydrochloride |
n-(3-(3-(n(1)-piperidinylmethyl)phenoxy)propyl)acetoxyacetamide |
n-(3-((alpha-piperidino-m-tolyl)oxy)propyl)glycolamide acetate (ester), monohydrochloride |
acetamide, 2-(acetyloxy)-n-(3-(3-(1-piperidinylmethyl)phenoxy)propyl)-, monohydrochloride |
acetamide, 2-hydroxy-n-(3-(m-(piperidinomethyl)phenoxy)propyl)-, acetate (ester), hydrochloride |
smr000469144 |
MLS001401443 |
roxatidine acetate hcl |
D01467 |
93793-83-0 |
roxatidine acetate hydrochloride (jp17/usan) |
altat (tn) |
[2-oxidanylidene-2-[3-[3-(piperidin-1-ylmethyl)phenoxy]propylamino]ethyl] ethanoate hydrochloride |
acetic acid [2-oxo-2-[3-[3-(1-piperidinylmethyl)phenoxy]propylamino]ethyl] ester hydrochloride |
A844708 |
nsc 760384 |
hoe 062 [roxatidine] |
60426gor1e , |
roxatidine acetate hydrochloride [usan:jan] |
unii-60426gor1e |
cas-93793-83-0 |
tox21_112500 |
tox21_112954 |
dtxsid2046670 , |
dtxcid0026670 |
nsc-760384 |
pharmakon1600-01502334 |
nsc760384 |
pifatidine hydrochloride |
CHEMBL2104871 |
CCG-101016 |
2-acetoxy-n-[3-[3-(1-piperidinomethylphenoxy]propyl]acetamide hydrochloride |
FT-0630983 |
AB07712 |
S1880 |
AKOS015894912 |
HY-B0305A |
roxatidine (acetate hydrochloride) |
SCHEMBL667643 |
NC00266 |
tox21_112500_1 |
NCGC00167499-02 |
n-(3-((.alpha.-piperidino-m-tolyl)oxy)propyl)glycolamide acetate monohydrochloride |
roxatidine acetate hydrochloride [mi] |
roxatidine acetate hydrochloride [who-dd] |
roxatidine acetate hydrochloride [usan] |
roxatidine acetate hydrochloride [mart.] |
roxatidine acetate hydrochloride [jan] |
2-acetoxy-n-(3-(m-(1-piperidinylmethyl)phenoxy)propyl)acetamidehydrochloride |
2-(acetyloxy)-n-[3-[3-(1-piperidinyl-methyl)phenoxy]propyl]- acetamide monohydrochloride |
AC-26444 |
R0178 |
2-acetoxy-n-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]acetamide hydrochloride |
SR-01000763240-4 |
C90611 |
CHEBI:32107 |
2-oxo-2-((3-(3-(piperidin-1-ylmethyl)phenoxy)propyl)amino)ethyl acetate hydrochloride |
SW197646-3 |
[2-oxo-2-[3-[3-(piperidin-1-ylmethyl)phenoxy]propylamino]ethyl] acetate;hydrochloride |
mfcd00941429 |
)propylamino)ethyl acetate hydrochloride |
2-oxo-2-(3-(3-(piperidin-1-ylmethyl)phenoxy)propylamino)ethyl acetate hydrochloride |
2-oxo-2-(3-(3-(piperidin-1-ylmethyl)phenoxy |
AS-14306 |
BCP10517 |
2-oxo-2-[[3-[3-(1-piperidylmethyl)phenoxy]propyl]amino]ethyl acetate hydrochloride |
AMY8936 |
Q27263158 |
SY111342 |
2-oxo-2-((3-(3-(piperidin-1-ylmethyl)phenoxy)propyl)amino)ethylacetatehydrochloride |
Excerpt | Reference | Relevance |
---|---|---|
" In common with many other prodrugs, the parent substance is not detectable in either plasma or urine and therefore all pharmacokinetic studies have been evaluated using measurements of roxatidine." | ( Pharmacokinetics of roxatidine in healthy volunteers. Collins, JD; Pidgen, AW, 1988) | 0.27 |
" Plasma and urine samples were collected throughout the study for the pharmacokinetic assessment." | ( The pharmacodynamics and pharmacokinetics of multiple doses of the new H2-receptor antagonist, roxatidine acetate, in healthy men. Ho, I; Lassman, HB; Puri, SK; Sabo, R; Scheffler, MR, 1988) | 0.27 |
Excerpt | Reference | Relevance |
---|---|---|
" Furthermore, there was no interference in the bioavailability of roxatidine acetate 150 mg daily when administered alone or in combination with a meal or antacids." | ( Interaction of roxatidine acetate with antacids, food and other drugs. Labs, RA, 1988) | 0.27 |
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
Excerpt | Relevance | Reference |
---|---|---|
" Dosage adjustment of TZU-0460 is necessary in renal failure." | ( Pharmacokinetics of TZU-0460, a new H2-receptor antagonist, in patients with impaired renal function. Hara, H; Hattori, N; Ishida, Y; Nakamura, S; Ohta, H; Satoh, S; Takabatake, T; Ushiogi, Y; Yamamoto, Y, 1986) | 0.27 |
" In rats single or repeated dosing with roxatidine acetate did not influence drug metabolising enzymes in the liver nor did the drug show antiandrogenic activity in long term animal studies." | ( A review of the animal pharmacology of roxatidine acetate. Bickel, M; Herling, AW; Scholtholt, J, 1988) | 0.27 |
"In a series of double-blind randomised studies in normal volunteers with continuous intragastric pH monitoring, the effects of different dosage regimens of roxatidine acetate, a new H2-receptor antagonist, were compared with placebo and ranitidine." | ( The effects of roxatidine acetate on 24-hour intragastric acidity. Investigations in healthy volunteers and comparison with ranitidine and placebo. Kaufmann, D; Kempf, M; Merki, HS; Neumann, J; Röhmel, J; Scheurle, E; Walt, RP; Witzel, L, 1988) | 0.27 |
" After 14 days' treatment with roxatidine acetate substantial reductions in ulcer sizes had been obtained, in addition to healing rates of 87 to 89%, with no significant differences between the dosage regimens." | ( A comparison of roxatidine acetate 150 mg once daily and 75 mg twice daily in duodenal ulcer healing. Hentschel, E; Schütze, K, 1988) | 0.27 |
Class | Description |
---|---|
piperidines | |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
acetylcholinesterase | Homo sapiens (human) | Potency | 30.9008 | 0.0025 | 41.7960 | 15,848.9004 | AID1347395 |
AR protein | Homo sapiens (human) | Potency | 22.0180 | 0.0002 | 21.2231 | 8,912.5098 | AID743035; AID743063 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 0.3202 | 0.0002 | 29.3054 | 16,493.5996 | AID743069; AID743075; AID743077; AID743079 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 13.8029 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 13.3322 | 0.0010 | 19.4141 | 70.9645 | AID743191 |
geminin | Homo sapiens (human) | Potency | 0.3548 | 0.0046 | 11.3741 | 33.4983 | AID624297 |
Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 18.8336 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 0.7079 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 26 (68.42) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 1 (2.63) | 29.6817 |
2010's | 5 (13.16) | 24.3611 |
2020's | 6 (15.79) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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 weak demand-to-supply ratio for research on this compound.
| This Compound (10.73) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 14 (36.84%) | 5.53% |
Reviews | 2 (5.26%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 22 (57.89%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |