GW 1100

生物活性靶点体外研究体内研究 GW 1100 试剂级价格

GW 1100

CAS号:306974-70-9
英文名:GW-1100
中文名:GW 1100
CBNumber:CB01872299
分子式:C27H25FN4O4S
分子量:520.58
MOL File:306974-70-9.mol

GW 1100化学性质

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 :Soluble in DMSO (up to 2 mg/ml) or in DMF (up to 5 mg/ml).
形态 :White powder
酸度系数(pKa) :1.20±0.22(Predicted)
颜色 :White
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20° for up to 3 months. Dilutions into aqueous media are not stable and should be used within one working day.

GW 1100性质、用途与生产工艺

生物活性 GW-1100是选择性的 GPR40 拮抗剂，pIC50为6.9。
靶点

pIC50: 6.9 (GPR40)
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.