GLPG0974
目录号 : GC31614An antagonist of FFAR2/GPR43
Cas No.:1391076-61-1
Sample solution is provided at 25 µL, 10mM.
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)
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. |
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 |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 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。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet