中文名 | GW-1100 |
英文名 | GW-1100 |
别名 | 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 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 |
英文别名 | GW1100 GW-1100 GW 1100 1-(4-Ethoxycarbonylphenyl)-2-(4-fluorobenzylthio)-5-(2-ethoxy-5-pyrimidinylmethyl)-4-pyrimidinone Benzoic acid, 4-[5-[(2-ethoxy-5-pyrimidinyl)methyl]-2-[[(4-fluorophenyl)methyl]thio]-4-oxo-1(4H)-pyrimidinyl]-, ethyl ester |
CAS | 306974-70-9 |
化学式 | C27H25FN4O4S |
分子量 | 520.58 |
密度 | 1.29±0.1 g/cm3(Predicted) |
熔点 | 208-210℃ |
沸点 | 690.2±65.0 °C(Predicted) |
溶解度 | 溶于DMSO (高达2 mg/ml) 或DMF (高达5 mg/ml)。 |
酸度系数 | 1.20±0.22(Predicted) |
存储条件 | +2C to +8C |
稳定性 | 从提供的购买之日起稳定1年。在DMSO或DMF中的溶液可以在-20 ℃ 下储存长达3个月。稀释到水介质中不稳定,应在一次工作中使用 |
外观 | 白色粉末 |
颜色 | White |
体外研究 | 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). |
体内研究 | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.921 ml | 9.604 ml | 19.209 ml |
5 mM | 0.384 ml | 1.921 ml | 3.842 ml |
10 mM | 0.192 ml | 0.96 ml | 1.921 ml |
5 mM | 0.038 ml | 0.192 ml | 0.384 ml |
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