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GS-9667

Catalog No. T27439   CAS 618380-90-8
Synonyms: CVT-3619, CVT 3619

GS-9667, a selective and partial agonist of the A(1) adenosine receptor (AR), represents an effective therapy for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA).

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GS-9667 Chemical Structure
GS-9667, CAS 618380-90-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 133.00
5 mg In stock $ 320.00
10 mg In stock $ 470.00
25 mg In stock $ 772.00
50 mg In stock $ 1,080.00
100 mg In stock $ 1,460.00
500 mg In stock $ 2,920.00
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Purity: 99.76%
ee: 100%
Purity: 99.76%
ee: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GS-9667, a selective and partial agonist of the A(1) adenosine receptor (AR), represents an effective therapy for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA).
In vivo In the single ascending dose study, healthy, non-obese, and obese subjects received GS-9667 (30-1,800 mg; oral; single dose). In the multiple, ascending dose study, healthy, obese subjects received GS-9667 (600-2,400 mg QD, 1,200 mg BID, or 600 mg QID) for 14 days. Doses of GS-9667 ≥300 mg caused dose-dependent reductions in FFA levels that were reproducible over 14 days without evidence of desensitization or rebound. All doses were well tolerated. GS-9667 was rapidly absorbed and distributed; Steady-state concentrations were achieved within 3-5 days. The A(1) AR partial agonist GS-9667 reduced plasma FFA, exhibited linear kinetics, and was well-tolerated in healthy non-obese and obese subjects.[1]
Synonyms CVT-3619, CVT 3619
Molecular Weight 461.51
Formula C21H24FN5O4S
CAS No. 618380-90-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (119.17 mM)

TargetMolReferences and Literature

1. Staehr PM, et al. Reduction of free fatty acids, safety, and pharmacokinetics of oral GS-9667, an A(1) adenosine receptor partial agonist. J Clin Pharmacol. 2013;53(4):385-392. 2. Yang M, et al. Adenosine A₁ receptors do not play a major role in the regulation of lipogenic gene expression in hepatocytes. Eur J Pharmacol. 2012;683(1-3):332-339. 3. Jiang Y, et al. Structural analysis, virtual screening and molecular simulation to identify potential inhibitors targeting 2'-O-ribose methyltransferase of SARS-CoV-2 coronavirus. J Biomol Struct Dyn. 2022;40(3):1331-1346. 4. Bergman RN, et al. Hypothesis: Role of Reduced Hepatic Insulin Clearance in the Pathogenesis of Type 2 Diabetes [published correction appears in Diabetes. 2019 Dec;68(12):2350]. Diabetes. 2019;68(9):1709-1716.

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Membrane Protein-targeted Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

GS-9667 618380-90-8 GPCR/G Protein Neuroscience Adenosine Receptor CVT3619 CVT-3619 CVT 3619 GS9667 GS 9667 inhibitor inhibit

 

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