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GW-1100

Catalog No. T15448 CAS 306974-70-9

GW-1100 is a selective antagonist of GPR40 (pIC50: 6.9). GW1100 also plays the role of a GPR40 inverse agonist.

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GW-1100, CAS 306974-70-9

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Description	GW-1100 is a selective antagonist of GPR40 (pIC50: 6.9). GW1100 also plays the role of a GPR40 inverse agonist.
Targets&IC50	FFA1/GPR40:(pic50)6.9
In vitro	GW-1100 (1 μM) produces a significant rightward shift in the concentration-response curve to GW9508 (pEC50=7.17±0.08 in the absence and pEC50=6.79±0.09 in the presence of 1 μM GW-1100; P<0.05; n=3). At concentrations of GW-1100 (3 μM and higher) shows a significant decrease in the maximal response is observed with a continuing rightward shift in the pEC50 response[2]. CHO-K1/bFFAR1 cells are incubated for 15 min with 10 μM GW1100 or vehicle (0.1% DMSO) and then stimulated with vehicle, oleic acid, linoleic acid or GW9508. GW-1100 significantly reduces the increase in intracellular calcium induced by 300 μM oleic acid (AUC(60-150 s), p<0.05), 100 μM linoleic acid (AUC(60-150 s), p<0.05) and 10 μM GW9508 (AUC(60-150 s), p<0.05)[3]. GW-1100 dose dependently suppresses GPR40-mediated Ca2+ elevations stimulated by GW9508 and linoleic acid (pIC50: 5.99±0.03 and 5.99±0.06, respectively). GW-1100 causes FFAR1 ligand-induced intracellular calcium in CHO-K1/bFFAR1 cells and neutrophils.
In vivo	These effects are inhibited by intracerebroventricular pretreatment with GW-1100 (10 μg), a GPR40 antagonist. The intracerebroventricular injection of DHA (50 μg) and GW9508 (1.0 μg) are a GPR40-selective agonist. This obviously decreases mechanical allodynia and thermal hyperalgesia on day 7, but not on day 1, after CFA injection[4].

Molecular Weight	520.58
Formula	C27H25FN4O4S
CAS No.	306974-70-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (96.05 mM), Sonication is recommended.

References and Literature

1. Stoddart LA, et al. Uncovering the pharmacology of the G protein-coupled receptor GPR40: high apparent constitutive activity in guanosine 5'-O-(3-[35S]thio)triphosphate binding studies reflects binding of an endogenous agonist. Mol Pharmacol. 2007 Apr;71( 2. Briscoe CP, et al. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol. 2006 Jul;148(5):619-28. 3. Manosalva C, et al. Cloning, identification and functional characterization of bovine free fatty acid receptor-1 (FFAR1/GPR40) in neutrophils. PLoS One. 2015 Mar 19;10(3):e0119715. 4. Nakamoto K, et al. Hypothalamic GPR40 signaling activated by free long chain fatty acids suppresses CFA-induced inflammatorychronic pain. PLoS One. 2013 Dec 12;8(12):e81563.

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Keywords

GW-1100 306974-70-9 Endocrinology/Hormones GPCR/G Protein GPR GW1100 GW 1100 inhibitor inhibit

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