MedKoo Cat#: 563495 | Name: GSK256073 Tris

Description:

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

GSK256073 is an agonist of G-protein coupled receptor 109A (GPR109A). It acts by reducing serum glucose in subjects with type 2 diabetes mellitus.

Chemical Structure

GSK256073 Tris
GSK256073 Tris
CAS#1228650-42-7 (tris)

Theoretical Analysis

MedKoo Cat#: 563495

Name: GSK256073 Tris

CAS#: 1228650-42-7 (tris)

Chemical Formula: C14H24ClN5O5

Exact Mass: 256.0727

Molecular Weight: 377.83

Elemental Analysis: C, 44.51; H, 6.40; Cl, 9.38; N, 18.54; O, 21.17

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.
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Synonym
GSK256073; GSK-256073; GSK 256073; GSK256073 Tris;
IUPAC/Chemical Name
8-chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dione compound with 2-amino-2-(hydroxymethyl)propane-1,3-diol (1:1)
InChi Key
HNAXNEBDLULUPW-UHFFFAOYSA-N
InChi Code
InChI=1S/C10H13ClN4O2.C4H11NO3/c1-2-3-4-5-15-7-6(12-9(11)13-7)8(16)14-10(15)17;5-4(1-6,2-7)3-8/h2-5H2,1H3,(H,12,13)(H,14,16,17);6-8H,1-3,5H2
SMILES Code
NC(CO)(CO)CO.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
>3 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

Preparing Stock Solutions

The following data is based on the product molecular weight 377.83 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
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. Epub 2015 Mar 12. 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. Epub 2015 Mar 13. 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. Epub 2013 Jun 12. PubMed PMID: 23701262.