替米沙坦
| CAS号 | 144701-48-4 | 货号 | BCP04513 |
| 中文名 | 替米沙坦 | ||
| 英文名 | Telmisartan | ||
| 中文别名 | |||
| 英文别名 | TU-199;TU 199;TU199; | ||
| 分子式 | C33H30N4O2 | 分子量 | 514.63 |
| 生物活性 | in vitro: In intact RVSMC cells and in membrane preparations, telmisartan inhibits the binding of 125I-AngII to AT1 receptors in a concentrationdependent manner, with an IC50 of 9.2 ±0.8 nM. The specific binding of [3H]telmisartan to SMC membranes is displaced by unlabeled telmisartan with an IC50 of 7.7± 1.8 nM and by cold AngII with an IC50 of 32.7 5.7 nM. Telmisartan directly prevents angiotensin II (Ang II)-induced endothelial dysfunction (ED) via activating HGF/Met system and/or PPARγ pathway . In cells treated with telmisartan (0.5-2.5 μmol/L) during exposure t non-uniform shear stress, dose-dependent inhibition of monocytic cell adhesion was observed, with about 45% reduction at 1 μmol/L . in vivo: Nine-week-old male db/db mice were fed a 60% high-fat diet, with orally administrated either vehicle (carboxymethyl-cellulose, CMC), 5 mg/kg telmisartan, or 5 mg/kg telmisartan and 1 mg/kg GW9662, a selective irreversible antagonist of PPARγ, for 5 weeks. Effects of telmisartan on Sir | ||
| 信号通路 | GPCR/G Protein | ||
| 靶 点 | Angiotensin Receptor | ||
结构式
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