306974-70-9

中文名称 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

英文名称 GW-1100

CAS 306974-70-9

分子式 C27H25FN4O4S

分子量 520.58

MOL 文件 306974-70-9.mol

306974-70-9 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

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

GW-1100
GW1100
GW1100
GPR40 Antagonist, GW1100 - CAS 306974-70-9 - Calbiochem
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

所属类别

生物化工：激动剂抑制剂

物理化学性质

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

溶解度可溶于 DMSO（高达 2 mg/ml）或 DMF（高达 5 mg/ml）。

酸度系数(pKa)1.20±0.22(Predicted)

形态白色粉末

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。

常见问题列表

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.