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371830

GPR40 Antagonist, GW1100

Name: GPR40 Antagonist, GW1100
Brand: MM

The GPR40 Antagonist, GW1100, also referenced under CAS 306974-70-9, controls the biological activity of GPR40. This small molecule/inhibitor is primarily used for Biochemicals applications.

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Synonym(s):

GPR40 Antagonist, GW1100, 1-(4-Ethoxycarbonylphenyl)-2-(4-fluorobenzylthio)-5-(2-ethoxy-5-pyrimidinylmethyl)-4-pyrimidinone, SB376752

Empirical Formula (Hill Notation):

C₂₇H₂₅FN₄O₄S

CAS Number:

306974-70-9

Molecular Weight:

520.58

MDL number:

MFCD09953714

Quality Level

100

Assay

≥97% (HPLC)

form

powder

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 50 mg/mL

shipped in

wet ice

storage temp.

2-8°C

SMILES string

FC(C=C1)=CC=C1CSC(N(C2=CC=C(C(OCC)=O)C=C2)C=C3CC4=CN=C(N=C4)OCC)=NC3=O

InChI

1S/C27H25FN4O4S/c1-3-35-25(34)20-7-11-23(12-8-20)32-16-21(13-19-14-29-26(30-15-19)36-4-2)24(33)31-27(32)37-17-18-5-9-22(28)10-6-18/h5-12,14-16H,3-4,13,17H2,1-2H3

InChI key

PTPNCCWOTBBVJR-UHFFFAOYSA-N

General description

A cell-permeable pyrimidinylmethyl-pyrimidinone compound that acts as potent, reversible and non-competitive GPR40 antagonist. Selectively blocks GPR40-mediated intracellular Ca²⁺ release stimulated by GPR40 Agonist GW9508 (Cat. No. 371706) and linoleic acid (pIC₅₀ of 5.99 in GPR40 expressing HEK293 cells) with no effect on GPR120-mediated activation. Shown to significantly reverse glucose-induced insulin secretion potentiated by GW9508 and only partially reduce linoleic acid effect in MIN6 cells.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Stoddart, L.A., et al. 2007. Mol. Pharmacol.71, 994.
Briscoe, C.P., et al. 2006. Br. J. Pharmacol.148, 619.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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CPL207280, a Novel G Protein-Coupled Receptor 40/Free Fatty Acid Receptor 1-Specific Agonist, Shows a Favorable Safety Profile and Exerts Antidiabetic Effects in Type 2 Diabetic Animals.

Katarzyna Bazydlo-Guzenda et al.

Molecular pharmacology, 100(4), 335-347 (2021-08-06)

G protein-coupled receptor (GPR) 40 is a free fatty acid receptor mainly expressed in pancreatic β-cells activated by medium- and long-chain fatty acids and regulating insulin secretion via an increase in cytosolic free calcium ([Ca2+]i). Activation of GPR40 in pancreatic

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