CAS 1001645-58-4|SRT1720 HCl
Introduction：Basic information about CAS 1001645-58-4|SRT1720 HCl, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | SRT1720 HCl | ||
|---|---|---|---|
| CAS Number | 1001645-58-4 | Molecular Weight | 506.022 |
| Density | 1.58 | Boiling Point | / |
| Molecular Formula | C25H23N7OS.xHCl | Melting Point | / |
| MSDS | / | Flash Point | / |
Names
| Name | N-[2-[3-(piperazin-1-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]quinoxaline-2-carboxamide,hydrochloride |
|---|---|
| Synonym | More Synonyms |
SRT1720 HCl BiologicalActivity
| Description | SRT 1720 Hydrochloride is a selective activator of SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities on SIRT2 and SIRT3 with EC1.5s of 37 μM and 300 μM, respectively. |
|---|---|
| Related Catalog | Signaling Pathways >>Autophagy >>AutophagySignaling Pathways >>Cell Cycle/DNA Damage >>SirtuinSignaling Pathways >>Epigenetics >>SirtuinResearch Areas >>Metabolic Disease |
| Target | SIRT1:0.16 μM (EC1.5) SIRT2:37 μM (EC1.5) |
| In Vitro | SRT1720 effectively decreases the acetylation of p53 in cells even in the absence of SIRT1, and this is attributed to inhibition of histone acetyltransferase p300[2]. |
| In Vivo | SRT1720 (10, 30, 100 mg/kg, p.o.) significantly reduces the hyperinsulinaemia after 4 weeks, partially normalizing elevated insulin levels similar to rosiglitazone treatment. SRT1720 treatment significantly reduces fasting blood glucose to near normal levels in Lepob/ob mice[1]. SRT1720 has ability to protect against the negative effects of diet-induced obesity in mice, and has a connection to metabolic adaptation in fatty acid and oxidative metabolism through downstream targets of SIRT1 such as PGC1α and FOXO1[2]. SRT1720 (50-100 mg/kg, p.o.), during emphysema development attenuates elastase-induced airspace enlargement and lung function impairment as well as reduces arterial oxygen saturation in WT mice[3]. |
| Animal Admin | Mice: Nine week old C57BL/6 male mice are fed a high fat diet (60% calories from fat) until their mean body weight reach approximately 40 g. The mice are then divided into test groups (6-10 per group). SRT1460 (100 mg/kg), SRT1720 (100 mg/kg), SRT501 (500 mg/kg) and rosiglitazone (5 mg/kg) are administered once daily via oral gavage. The vehicle used is 2% HPMC + 0.2% DOSS. Individual mouse body weights are measured twice weekly. At 2, 4, 6, 8 and 10 weeks of dosing a fed blood glucose measure is taken and after 5 weeks of treatment an IPGTT is conducted on all mice from each of the groups. After 10 weeks of treatment, an ITT is conducted. Statistical analysis is completed using the JMP program. Data are analyzed by a one way ANOVA with comparison to control using a Dunnett’s Test. A p value < 0.05 indicates a significant difference between groups. |
| References | [1]. Milne JC et al. Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes. Nature. 2007 Nov 29;450(7170):712-6 [2]. Baur JA, et al. Are sirtuins viable targets for improving healthspan and lifespan?,Nat Rev Drug Discov. 2012 Jun 1;11(6):443-61 [3]. Yao H, et al. SIRT1 protects against emphysema via FOXO3-mediated reduction of premature senescence in mice.,J Clin Invest. 2012 Jun 1;122(6):2032-45. [4]. Gao D, et al. Activation of SIRT1 Attenuates Klotho Deficiency-Induced Arterial Stiffness and Hypertension by Enhancing AMP-Activated Protein Kinase Activity. Hypertension. 2016 Nov;68(5):1191-1199. |
Chemical & Physical Properties
| Density | 1.58 |
|---|---|
| Molecular Formula | C25H23N7OS.xHCl |
| Molecular Weight | 506.022 |
| Exact Mass | 505.145142 |
| PSA | 115.69000 |
| LogP | 4.80520 |
| InChIKey | DTGRRMPPXCRRIM-UHFFFAOYSA-N |
| SMILES | Cl.O=C(Nc1ccccc1-c1cn2c(CN3CCNCC3)csc2n1)c1cnc2ccccc2n1 |
Safety Information
| Hazard Codes | Xi |
|---|---|
| HS Code | 2934100090 |
Customs
| HS Code | 2934100090 |
|---|---|
| Summary | 2934100090 other compounds containing an unfused thiazole ring (whether or not hydrogenated) in the structure VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0% |
Synonyms
| SRT1720 |
| 2-Quinoxalinecarboxamide, N-[2-[3-(1-piperazinylmethyl)imidazo[2,1-b]thiazol-6-yl]phenyl]-, hydrochloride (1:1) |
| SRT-1720,SRT 1720 |
| QCR-61 |
| SRT 1720 Hydrochloride |
| N-{2-[3-(1-Piperazinylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl}-2-quinoxalinecarboxamide hydrochloride (1:1) |
| cc-265 |
| CS-0509 |
| S1129_Selleck |
| N-[2-[3-(1-Piperazinylmethyl)imidazo[2,1-b]thiazol-6-yl]phenyl]-2-quinoxalinecarboxamide hydrochloride |
| SRT 1720 |
| SRT 1720 (Hydrochloride) |
