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371830

Sigma-Aldrich

GPR40 Antagonist, GW1100

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:
Molecular Weight:
520.58
MDL number:

Quality Level

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

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371721371706346003
GPR40 Antagonist, GW1100 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.

371830

GPR40 Antagonist, GW1100

GPR40 Agonist II The GPR40 Agonist II controls the biological activity of GPR40. This small molecule/inhibitor is primarily used for Biochemicals applications.

371721

GPR40 Agonist II

GPR40 Agonist The GPR40 Agonist, also referenced under CAS 885101-89-3, controls the biological activity of GPR40. This small molecule/inhibitor is primarily used for Cell Signaling applications.

371706

GPR40 Agonist

Glucagon Receptor Antagonist II The Glucagon Receptor Antagonist II, also referenced under CAS 191034-25-0, controls the biological activity of Glucagon Receptor.

346003

Glucagon Receptor Antagonist II

assay

≥97% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

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

11 - Combustible Solids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


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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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