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MK-2305

(CAS: 905723-46-8 )

Suppliers of MK-2305

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AMEDCHEM [email protected] +862168061059 CHINA

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Background Information of MK-2305

MK-2305 is a non-carboxylate GPR40 agonist. GPR40, also known as FFAR1, belongs to the class A family of G-protein coupled receptors, and is expressed predominantly in pancreatic β cells and enteroendocrine cells.GPR40 partial agonism is a promising new mechanism for the treatment of type 2 diabetes mellitus with clinical proof of concept. 

Solubility of MK-2305

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Mechanism and Indications

Signaling Pathways GPCR/G Protein
Target GPR40
Research Area Metabolic Disease
Indications

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase

Chemical Information

M.Wt Formula CAS No. Synonyms
443.82 C19H13ClF3NO4S 905723-46-8

Structure Information of MK-2305

Smiles C1C(C(F)(F)F)=CC(Cl)=C(OC2=CC3OCC[[email protected]](C4SC(=O)NC4=O)([H])C=3C=C2)C=1 |&1:17|
InChI InChI=1S/C19H13ClF3NO4S/c20-13-7-9(19(21,22)23)1-4-14(13)28-10-2-3-11-12(5-6-27-15(11)8-10)16-17(25)24-18(26)29-16/h1-4,7-8,12,16H,5-6H2,(H,24,25,26)/t12-,16?/m1/s1

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M-I C19H22O5S 0
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GPR40 agonist 1 1312788-44-5 C24H20O3 0
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Chemical and Physical Properties

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Reference

[1].Huang H, et al. Discovery of novel benzo[b]thiophene tetrazoles as non-carboxylate GPR40 agonists. Bioorg Med Chem Lett. 2017 Dec 12. pii: S0960-894X(17)31182-4.
GPR40 partial agonism is a promising new mechanism for the treatment of type 2 diabetes mellitus with clinical proof of concept. Most of the GPR40 agonists in the literature have a carboxylic acid functional group, which may pose a risk for idiosyncratic drug toxicity. A novel series of GPR40 agonists containing a tetrazole as a carboxylic acid bioisostere was identified. This series of compounds features a benzo[b]thiophene as the center ring, which is prone to oxidation during phase 1 metabolism. Following SAR optimization targeting GPR40 agonist activity and intrinsic clearance in microsomes (human and rat), potent and metabolically stable compounds were selected for in vivo evaluation. The compounds are efficacious at lowering blood glucose in a SD rat oGTT model.

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