GSK256073 | CAS#862892-90-8 | GPCR Agonist

MedKoo Cat#: 531872 | Name: GSK256073

Description:

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

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.

Chemical Structure

GSK256073

CAS#862892-90-8 (free)

Theoretical Analysis

MedKoo Cat#: 531872

Name: GSK256073

CAS#: 862892-90-8 (free)

Chemical Formula: C10H13ClN4O2

Exact Mass: 256.0727

Molecular Weight: 256.69

Elemental Analysis: C, 46.79; H, 5.10; Cl, 13.81; N, 21.83; O, 12.47

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

Bulk Inquiry

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

Instruction

View handling instruction

Preparing Stock Solutions

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

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.