A selective GPR40 antagonist
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GW 1100

Item No. 10008908

Technical Information
Formal Name
4-[5-[(2-ethoxy-5-pyrimidinyl)methyl]-2-[[(4-fluorophenyl)methyl]thio]-4-oxo-1(4H)-pyrimidinyl]-benzoic acid, ethyl ester
CAS Number
306974-70-9
Molecular Formula
C27H25FN4O4S
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMF: 5 mg/mlDMF:PBS (pH 7.2) (1:4): 0.20 mg/mlDMSO: 2 mg/ml
λmax
243 nm
SMILES
FC1=CC=C(CSC(N(C2=CC=C(C(OCC)=O)C=C2)C=C3CC4=CN=C(OCC)N=C4)=NC3=O)C=C1
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    GW 1100 is a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells stimulated by GW 9508 (an agonist of both GPR40 and GPR120 (FFAR4), another GPCR activated by long chain fatty acids) or linoleic acid with a pIC50 value equal to 5.99. However at concentrations up to 10 μM, GW 1100 has no effect on GPR120-mediated stimulation of intracellular Ca2+ release induced by either GW 9508 or linoleic acid.1 In the MIN6 mouse insulinoma cell line, 1 μM GW 1100 inhibits the potentiating effects of GW 9508 and linoleic acid on glucose-stimulated insulin secretion.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Briscoe, C.P., Peat, A.J., McKeown, S.C., et alPharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: Identification of agonist and antagonist small molecules. Br. J. Pharmacol. 148(5), 619-628 (2006).

    Product Citations

    Matsumoto, N., Singh, N., Lee, K.S., et alThe epoxy fatty acid pathway enhances cAMP in mammalian cells through multiple mechanisms. Prostaglandins Other Lipid Mediat. 162, 106662 (2022).