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GLPG0974

目录号 : GC31614

An antagonist of FFAR2/GPR43

GLPG0974 Chemical Structure

Cas No.:1391076-61-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,547.00
现货
5mg
¥1,450.00
现货
10mg
¥2,320.00
现货
25mg
¥4,410.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

GLPG0974 is an antagonist of free fatty acid receptor 2 (FFAR2/GPR43; IC50 = 9 nM).1 It is selective for FFAR2 over FFAR3 at concentrations up to 30 μM and over a panel of 55 receptors, ion channels, and transporters at 10 μM. GLPG0974 inhibits acetate-induced migration of isolated human neutrophils in buffer or plasma (IC50s = 27 and 43 nM, respectively), as well as acetate-induced expression of CD11b activation-specific epitope on neutrophils in isolated human whole blood (IC50 = 438 nM). GLPG0974 also inhibits a human FFAR2-based designer receptor exclusively activated by designer drugs (hFFAR2-DREADD; IC50 = 36.31 nM in a cell-based β-arrestin-2 recruitment assay).2 It inhibits glucagon-like peptide 1 (GLP-1) secretion induced by the hFFA2-DREADD ligand sorbic acid in isolated colonic crypts from mice expressing hemagglutinin-tagged hFFAR2-DREADD when used at a concentration of 10 μM.

1.Pizzonero, M., Dupont, S., Babel, M., et al.Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: From hit to clinicJ. Med. Chem.57(23)10044-10057(2014) 2.Bolognini, D., Barki, N., Butcher, A.J., et al.Chemogenetics defines receptor-mediated functions of short chain free fatty acidsNat. Chem. Biol.15(5)489-498(2019)

实验参考方法

Animal experiment:

Rats[1]GLPG0974 is orally dosed as a single esophageal gavage at 5−10 mg/kg and intravenously dosed as a bolus via the caudal vein at 1 mg/kg to male Sprague−Dawley rats. Each group consisted of three rats. Blood samples are collected[1].

References:

[1]. Pizzonero M, et al. Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic. J Med Chem. 2014 Dec 11;57(23):10044-57.

化学性质

Cas No. 1391076-61-1 SDF
化学名 4-[[[(2R)-1-(benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)methyl]amino]-butanoic acid
Canonical SMILES O=C(O)CCCN(C([C@]1(C)N(C(C2=CSC3=CC=CC=C32)=O)CC1)=O)CC4=CC=CC(Cl)=C4
分子式 C25H25ClN2O4S 分子量 485
溶解度 DMSO : 200 mg/mL (412.37 mM; Need ultrasonic) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.0619 mL 10.3093 mL 20.6186 mL
5 mM 0.4124 mL 2.0619 mL 4.1237 mL
10 mM 0.2062 mL 1.0309 mL 2.0619 mL
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