GW 1100
| 中文名称 | GW 1100 |
|---|---|
| 中文同义词 | 4-[5-[(2-乙氧基-5-嘧啶)甲基]-2-[[(4-氟苯基)甲基]硫代]-4-氧代-1(4H)-嘧啶]-苯甲酸乙酯;1-(4-乙氧羰基苯基)-2-(4-氟苄基硫基)-5-(2-乙氧基-5-嘧啶基甲基)-4-嘧啶酮 |
| 英文名称 | GW-1100 |
| 英文同义词 | Benzoic acid, 4-[5-[(2-ethoxy-5-pyrimidinyl)methyl]-2-[[(4-fluorophenyl)methyl]thio]-4-oxo-1(4H)-pyrimidinyl]-, ethyl ester;GW-1100;1-(4-Ethoxycarbonylphenyl)-2-(4-fluorobenzylthio)-5-(2-ethoxy-5-pyrimidinylmethyl)-4-pyrimidinone;GPR40 Antagonist, GW1100 - CAS 306974-70-9 - Calbiochem;GW1100;GW1100 |
| CAS号 | 306974-70-9 |
| 分子式 | C27H25FN4O4S |
| 分子量 | 520.58 |
| EINECS号 | |
| 相关类别 | G蛋白偶联受体&G蛋白;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Aromatics;Heterocycles |
| Mol文件 | 306974-70-9.mol |
| 结构式 |  |
GW 1100 性质
| 熔点 | 208-210℃ |
|---|---|
| 沸点 | 690.2±65.0 °C(Predicted) |
| 密度 | 1.29±0.1 g/cm3(Predicted) |
| 储存条件 | +2C to +8C |
| 溶解度 | 可溶于 DMSO（高达 2 mg/ml）或 DMF（高达 5 mg/ml）。 |
| 形态 | 白色粉末 |
| 酸度系数(pKa) | 1.20±0.22(Predicted) |
| 颜色 | 白色 |
| 稳定性 | 可在-20°下的DMSO或DMF中的溶液储存长达3个月。稀释到水性介质中不稳定，应在一个工作日内使用。 |
pIC50: 6.9 (GPR40)
GW-1100 (GW1100) dose dependently inhibits GPR40-mediated Ca 2+ elevations stimulated by GW9508 and linoleic acid (pIC 50 values of 5.99±0.03 and 5.99±0.06, respectively). GW-1100 at a concentration of 1 μM produces a significant rightward shift in the concentration-response curve to GW9508 (pEC 50 =7.17±0.08 in the absence and pEC 50 =6.79±0.09 in the presence of 1 μM GW-1100; P<0.05; n=3). At concentrations of GW-1100 of 3 μM and higher a significant decrease in the maximal response is observed with a continuing rightward shift in the pEC 50 response. GW-1100 (GW1100) reduces FFAR1 ligand-induced intracellular calcium in CHO-K1/bFFAR1 cells and neutrophils. 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).
The intracerebroventricular injection of DHA (50 µg) and GW9508 (1.0 µg), a GPR40-selective agonist, significantly reduces mechanical allodynia and thermal hyperalgesia at day 7, but not at day 1, after CFA injection. These effects are inhibited by intracerebroventricular pretreatment with GW-1100 (10 µg), a GPR40 antagonist.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-50691 | GW-1100 | 1 mg | 249元 | |
| 2024/01/25 | HY-50691 | 4-[5-[(2-乙氧基-5-嘧啶)甲基]-2-[[(4-氟苯基)甲基]硫代]-4-氧代-1(4H)-嘧啶]-苯甲酸乙酯 GW-1100 | 306974-70-9 | 5mg | 549元 |