GS-9667

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 525177

CAS#: 618380-90-8

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

Chemical Structure

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GS-9667
CAS# 618380-90-8
Instruction

Theoretical Analysis

MedKoo Cat#: 525177
Name: GS-9667
CAS#: 618380-90-8
Chemical Formula: C21H24FN5O4S
Exact Mass: 461.15
Molecular Weight: 461.510
Elemental Analysis: C, 54.65; H, 5.24; F, 4.12; N, 15.17; O, 13.87; S, 6.95

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: GS-9667; GS-9667; GS-9667; CVT 3619.

IUPAC/Chemical Name: (2S,3S,4R,5R)-2-(((2-fluorophenyl)thio)methyl)-5-(6-(((1R,2R)-2-hydroxycyclopentyl)amino)-9H-purin-9-yl)tetrahydrofuran-3,4-diol

InChi Key: IZRXENCTXNMAMI-DIJFLQFKSA-N

InChi Code: InChI=1S/C21H24FN5O4S/c22-11-4-1-2-7-15(11)32-8-14-17(29)18(30)21(31-14)27-10-25-16-19(23-9-24-20(16)27)26-12-5-3-6-13(12)28/h1-2,4,7,9-10,12-14,17-18,21,28-30H,3,5-6,8H2,(H,23,24,26)/t12-,13-,14-,17-,18-,21-/m1/s1

SMILES Code: c1ccc(c(c1)F)SC[C@@H]2[C@H]([C@H]([C@@H](O2)n3cnc4c3ncnc4N[C@@H]5CCC[C@H]5O)O)O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 461.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Staehr PM, Dhalla AK, Zack J, Wang X, Ho YL, Bingham J, Belardinelli L. Reduction of free fatty acids, safety, and pharmacokinetics of oral GS-9667, an A(1) adenosine receptor partial agonist. J Clin Pharmacol. 2013 Apr;53(4):385-92. doi: 10.1002/jcph.9. Epub 2013 Feb 20. PubMed PMID: 23427000.

2: Yang M, Chu R, Chisholm JW, Doege H, Belardinelli L, Dhalla AK. Adenosine A₁ receptors do not play a major role in the regulation of lipogenic gene expression in hepatocytes. Eur J Pharmacol. 2012 May 15;683(1-3):332-9. doi: 10.1016/j.ejphar.2012.03.012. Epub 2012 Mar 16. PubMed PMID: 22449383.

3: Shearer J, Severson DL, Su L, Belardinelli L, Dhalla AK. Partial A1 adenosine receptor agonist regulates cardiac substrate utilization in insulin-resistant rats in vivo. J Pharmacol Exp Ther. 2009 Jan;328(1):306-11. doi: 10.1124/jpet.108.143594. Epub 2008 Oct 24. PubMed PMID: 18952888.

4: Dhalla AK, Santikul M, Chisholm JW, Belardinelli L, Reaven GM. Comparison of the antilipolytic effects of an A1 adenosine receptor partial agonist in normal and diabetic rats. Diabetes Obes Metab. 2009 Feb;11(2):95-101. doi: 10.1111/j.1463-1326.2008.00902.x. Epub 2008 May 20. PubMed PMID: 18494808.

5: Dhalla AK, Wong MY, Voshol PJ, Belardinelli L, Reaven GM. A1 adenosine receptor partial agonist lowers plasma FFA and improves insulin resistance induced by high-fat diet in rodents. Am J Physiol Endocrinol Metab. 2007 May;292(5):E1358-63. Epub 2007 Jan 16. PubMed PMID: 17227958.

6: Dhalla AK, Santikul M, Smith M, Wong MY, Shryock JC, Belardinelli L. Antilipolytic activity of a novel partial A1 adenosine receptor agonist devoid of cardiovascular effects: comparison with nicotinic acid. J Pharmacol Exp Ther. 2007 Apr;321(1):327-33. Epub 2007 Jan 4. PubMed PMID: 17204748.

7: Fatholahi M, Xiang Y, Wu Y, Li Y, Wu L, Dhalla AK, Belardinelli L, Shryock JC. A novel partial agonist of the A(1)-adenosine receptor and evidence of receptor homogeneity in adipocytes. J Pharmacol Exp Ther. 2006 May;317(2):676-84. Epub 2006 Jan 12. PubMed PMID: 16410404.