SRT2104: a sirtuin 1 activator; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 25108829 |
| CHEMBL ID | 4297436 |
| SCHEMBL ID | 964014 |
| MeSH ID | M0589342 |
| Synonym |
|---|
| HY-15262 |
| CS-0955 |
| srt 2104 |
| S7792 |
| 1093403-33-8 |
| sirtuin modulator |
| SCHEMBL964014 |
| c26h24n6o2s2 |
| srt2104 (gsk2245840) |
| AC-33074 |
| 5-thiazolecarboxamide, 4-methyl-n-(2-(3-(4-morpholinylmethyl)imidazo(2,1-b)thiazol-6-yl)phenyl)-2-(3-pyridinyl)- |
| 4-methyl-n-(2-(3-morpholinomethyl)imidazo(2,1-b)thiazol-6-yl)phenyl-2-(pyridine-3-yl)thiazole-5-carboxamide |
| 4521NR0J09 , |
| srt2104 |
| unii-4521nr0j09 |
| 4-methyl-n-(2-(3-(morpholinomethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)-2-(pyridin-3-yl)thiazole-5-carboxamide |
| srt-2104 |
| DTXSID00648729 |
| 4-methyl-n-(2-{3-[(morpholin-4-yl)methyl]imidazo[2,1-b][1,3]thiazol-6-yl}phenyl)-2-(pyridin-3-yl)-1,3-thiazole-5-carboxamide |
| compound 4 [ng et al., 2013] |
| EX-A1287 |
| 4-methyl-n-[2-[3-(morpholin-4-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]-2-pyridin-3-yl-1,3-thiazole-5-carboxamide |
| gtpl9515 |
| AKOS030526247 |
| LAMQVIQMVKWXOC-UHFFFAOYSA-N |
| gsk2245840 |
| NCGC00379071-01 |
| 5-thiazolecarboxamide, 4-methyl-n-[2-[3-(4-morpholinylmethyl)imidazo[2,1-b]thiazol-6-yl]phenyl]-2-(3-pyridinyl)- |
| 4-methyl-n-[2-[3-(morpholinomethyl)imidazo[2,1-b]thiazol-6-yl]phenyl]-2-(pyridin-3-yl)thiazole-5-carboxamide |
| DB12186 |
| BCP17468 |
| 5-thiazolecarboxamide,4-methyl-n-(2-(3-(4-morpholinylmethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)-2-(3-pyridinyl)- |
| CCG-269826 |
| Q27258795 |
| CHEMBL4297436 |
| A921925 |
| AS-57311 |
SRT2104 is a novel, first-in-class, highly selective small-molecule activator of SIRT1. Its effect and mechanism unknown on DN.
| Excerpt | Reference | Relevance |
|---|---|---|
| "SRT2104 is a novel SIRT1 activator and was not previously studied for its effects on diabetes-induced aortic endothelial dysfunction." | ( SRT2104 attenuates diabetes-induced aortic endothelial dysfunction via inhibition of P53. Huang, W; Jia, Y; Li, Y; Wang, J; Wu, H; Wu, J; Zhang, H; Zhou, S, 2018) | 2.64 |
| "SRT2104 is a novel, first-in-class, highly selective small-molecule activator of SIRT1, with its effect and mechanism unknown on DN." | ( P53/NRF2 mediates SIRT1's protective effect on diabetic nephropathy. Huang, W; Jia, Y; Jiang, Z; Ma, F; Sun, W; Wu, H; Wu, J, 2019) | 1.24 |
| "SRT2104 is a selective activator of SIRT1. " | ( A phase II, randomized, placebo-controlled, double-blind, multi-dose study of SRT2104, a SIRT1 activator, in subjects with type 2 diabetes. Baksi, A; Elliott, P; Haddad, J; Hoffmann, E; Jacobson, EW; Kraydashenko, O; Stets, R; Vlasuk, GP; Zalevkaya, A, 2014) | 2.07 |
Treatment with SRT2104 did not lead to any consistent, dose-related changes in glucose or insulin. The observed pharmacokinetics were not dose proportional and had large between subject variability.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Treatment with SRT2104 did not lead to any consistent, dose-related changes in glucose or insulin." | ( A phase II, randomized, placebo-controlled, double-blind, multi-dose study of SRT2104, a SIRT1 activator, in subjects with type 2 diabetes. Baksi, A; Elliott, P; Haddad, J; Hoffmann, E; Jacobson, EW; Kraydashenko, O; Stets, R; Vlasuk, GP; Zalevkaya, A, 2014) | 0.97 |
| "Treatment with SRT2104 for 28 days did not result in improved glucose or insulin control which is likely due to the observed pharmacokinetics which were not dose proportional and had large between subject variability." | ( A phase II, randomized, placebo-controlled, double-blind, multi-dose study of SRT2104, a SIRT1 activator, in subjects with type 2 diabetes. Baksi, A; Elliott, P; Haddad, J; Hoffmann, E; Jacobson, EW; Kraydashenko, O; Stets, R; Vlasuk, GP; Zalevkaya, A, 2014) | 0.98 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " One subject experienced an SAE requiring study withdrawal and another was withdrawn for a severe UC flare; 19 subjects (61%) across both treatment groups experienced at least 1 treatment emergent adverse event." | ( Assessing Colonic Exposure, Safety, and Clinical Activity of SRT2104, a Novel Oral SIRT1 Activator, in Patients with Mild to Moderate Ulcerative Colitis. Freudenberg, JM; Haddad, J; Hoffmann, E; Jacobson, E; Joshi, S; McCallum, SW; Oommen, DE; Sands, BE, 2016) | 0.68 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "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 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 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. |
| AID1347160 | Primary screen NINDS Rhodamine 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. |
| 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. |
| 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. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| 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 | 12 (50.00) | 24.3611 |
| 2020's | 12 (50.00) | 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 moderate demand-to-supply ratio for research on this compound.
| This Compound (31.51) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 5 (20.83%) | 5.53% |
| Reviews | 1 (4.17%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 18 (75.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||