MedKoo Cat#: 555128 | Name: GSK2973980A

Description:

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

GSK2973980A is a potent and selective DGAT1 inhibitor (hDGAT1 LE IC50 = 3 nM). GSK2973980A demonstrates excellent DMPK profiles and in vivo efficacy in a postprandial lipid excursion model in mice. Based on the overall biological and developability profiles and acceptable safety profiles in the 7-day toxicity studies in rats and dogs, GSK2973980A was selected as a candidate compound for further development in the treatment of metabolic disorders.

Chemical Structure

GSK2973980A
GSK2973980A
CAS#1414797-35-5

Theoretical Analysis

MedKoo Cat#: 555128

Name: GSK2973980A

CAS#: 1414797-35-5

Chemical Formula: C25H19F5N4O4

Exact Mass: 534.1326

Molecular Weight: 34.44

Elemental Analysis: C, 56.18; H, 3.58; F, 17.77; N, 10.48; O, 11.97

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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Related CAS #
No Data
Synonym
GSK2973980A; GSK-2973980A; GSK 2973980A;
IUPAC/Chemical Name
(S)-2-(6-(5-(3-(3,4-difluorophenyl)ureido)pyrazin-2-yl)-1-oxo-2-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydronaphthalen-2-yl)acetic acid
InChi Key
OTKTZEZTFCAULO-DEOSSOPVSA-N
InChi Code
InChI=1S/C25H19F5N4O4/c26-17-4-2-15(8-18(17)27)33-23(38)34-20-11-31-19(10-32-20)14-1-3-16-13(7-14)5-6-24(22(16)37,9-21(35)36)12-25(28,29)30/h1-4,7-8,10-11H,5-6,9,12H2,(H,35,36)(H2,32,33,34,38)/t24-/m0/s1
SMILES Code
O=C(O)C[C@@](CCC1=C2C=CC(C3=NC=C(NC(NC4=CC=C(F)C(F)=C4)=O)N=C3)=C1)(CC(F)(F)F)C2=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
Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) plays an important role in triglyceride synthesis and is a target of interest for the treatment of metabolic disorders

Preparing Stock Solutions

The following data is based on the product molecular weight 34.44 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
Discovery of Tetralones as Potent and Selective Inhibitors of Acyl-CoA:Diacylglycerol Acyltransferase 1 Mui Cheung, Raghuram S. Tangirala, Sridhar R. Bethi, Hemant V. Joshi, Jennifer L. Ariazi, Vijaya G. Tirunagaru, and Sanjay Kumar Publication Date (Web): January 16, 2018 (Letter) DOI: 10.1021/acsmedchemlett.7b00450