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
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
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.
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.