Telmisartan 是一种血管紧张素II 1型受体拮抗剂，能够抑制其活性，IC50值为 9.2 nM。

Telmisartan is an Angiotensin 2 Receptor Blocker. The mechanism of action of telmisartan is as an Angiotensin 2 Receptor Antagonist.

在高碳水化合物、高脂肪喂养的小鼠中,Telmisartan使内脏脂肪的积聚减少,并使脂肪细胞大小降低,效果远大于缬沙坦,且与肝甘油三酯水平显著降低有关;Telmisartan还促进热量消耗的增加和防止饮食诱导的体重增加.

Telmisartan是有一定效果的选择性PPARγ部分激动剂（EC50= 4.5 μM）,对受体的激活效应达到完全激动剂吡格列酮和罗格列酮最高水平的25％-30％。在Hep3B细胞中,Telmisartan降低基底以及AGE诱导的RAGE蛋白表达,它还剂量依赖性地抑制AGE诱导的ROS产生,随后诱导CRP基因和蛋白的表达。在正在分化和完全分化的脂肪细胞中,Telmisartan剂量依赖性增加mRNA水平,如PPARgamma靶基因AP2和脂连蛋白。在分化脂肪细胞中,Telmisartan减弱1型11beta羟脱氢酶的mRNA水平。Telmisartan诱导3T3-L1细胞的脂肪分化。Telmisartan导致小鼠肌肉肌管中的ACC2的表达减少到60％-70％。 Telmisartan而非坎地沙坦（另一ARB）,剂量依赖性地下调RAGE mRNA水平。Telmisartan对3T3-L1前脂肪细胞的分化具有有效的促进作用。

Telmisartan is prepared as a 10 mM stock solution in DMSO. Cell proliferation is assayed using the CCK-8 cell counting kit. Briefly, 5×103 cells are seeded into each well of a 96-well plate and cultured in 100 μL of RPMI-1640 supplemented with 10% FBS. After 24 h, ARBs (telmisartan, irbesartan, losartan, and valsartan at 0, 1, 10, or 100 μM) or vehicle is added to each well, and cells are cultured for an additional 48 h. CCK-8 reagent (10 μL) is added to each well, and the plates are incubated at 37°C for 3 h. The absorbance is measured at 450 nm using a microplate reader.

144701-48-4

C33H30N4O2

514.629

BIBR 277;替米沙坦

DMSO:10.3 mg/mL (20 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years