WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H531872
CAS#: 862892-90-8 (free)
Description: GSK 256073 is a high affinity agonist of the G-protein coupled receptor (GPCR)-associated protein for the treatment of dyslipidaemia and type 2 diabetes mellitus.
Hodoodo Cat#: H531872
Name: GSK256073
CAS#: 862892-90-8 (free)
Chemical Formula: C10H13ClN4O2
Exact Mass: 256.07
Molecular Weight: 256.690
Elemental Analysis: C, 46.79; H, 5.10; Cl, 13.81; N, 21.83; O, 12.47
This product is not in stock, which may be available by custom synthesis.
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Related CAS #: 1228650-42-7 (tris) 862892-90-8 (free)
Synonym: GSK256073; GSK 256073; GSK-256073.
IUPAC/Chemical Name: 8-chloro-3-pentyl-7H-purine-2,6-dione
InChi Key: CGAMDQCXAAOFSR-UHFFFAOYSA-N
InChi Code: InChI=1S/C10H13ClN4O2/c1-2-3-4-5-15-7-6(12-9(11)13-7)8(16)14-10(15)17/h2-5H2,1H3,(H,12,13)(H,14,16,17)
SMILES Code: O=C(N1)N(CCCCC)C2=C(NC(Cl)=N2)C1=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: | |
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The following data is based on the product molecular weight 256.69 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.
| 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: |
1: Sprecher D, Maxwell M, Goodman J, White B, Tang CM, Boullay V, de Gouville AC. Discovery and characterization of GSK256073, a non-flushing hydroxy-carboxylic acid receptor 2 (HCA2) agonist. Eur J Pharmacol. 2015 Jun 5;756:1-7. doi: 10.1016/j.ejphar.2015.01.051. PubMed PMID: 25773497.
2: Dobbins R, Byerly R, Gaddy R, Gao F, Mahar K, Napolitano A, Ambery P, Le Monnier de Gouville AC. GSK256073 acutely regulates NEFA levels via HCA2 agonism but does not achieve durable glycaemic control in type 2 diabetes. A randomised trial. Eur J Pharmacol. 2015 May 15;755:95-101. doi: 10.1016/j.ejphar.2015.03.005. PubMed PMID: 25773496.
3: Dobbins RL, Shearn SP, Byerly RL, Gao FF, Mahar KM, Napolitano A, Nachbaur GJ, Le Monnier de Gouville AC. GSK256073, a selective agonist of G-protein coupled receptor 109A (GPR109A) reduces serum glucose in subjects with type 2 diabetes mellitus. Diabetes Obes Metab. 2013 Nov;15(11):1013-21. doi: 10.1111/dom.12132. PubMed PMID: 23701262.
