Telmisartan is a potent, long lasting antagonist ofangiotensin II type 1 receptor (AT1), selectively inhibiting the binding of¹²⁵I-AngII to AT1 receptors withIC₅₀of 9.2 nM.

IC50: 9.2 nM (angiotensin II type 1 receptor)^[1]

In intact RVSMC cells and in membrane preparations, telmisartan inhibits the binding of¹²⁵I-AngII to AT1 receptors in a concentration-dependent manner, with an IC₅₀of 9.2 ± 0.8 nM. In the same experimental conditions, angiotensin II displaces¹²⁵I-AngII with an IC₅₀value of 2.9 ± 0.5 nM. The specific binding of [³H]telmisartan to SMC membranes is displaced by unlabeled telmisartan with an IC₅₀of 7.7 ± 1.8 nM and by cold AngII with an IC₅₀of 32.7 ± 5.7 nM^[1]. Telmisartan treatment (100 μM) reduces the proliferation of three EAC cell lines (OE19, OE33, and SKGT-4), induces cell cycle arrest in G0/G1 phase and regulates cell cycle-related proteins in EAC cells, and induces the phosphorylation of AMPK and regulates cell cycle-related proteins via the AMPK/mTOR pathway in EAC cells. Telmisartan inhibits the activation of RTKs, downstream effectors and cell cycle-related proteins^[5].

In the telmisartan (0.1, 0.3, and 1 mg/kg)-treated rats, the specific binding of [³H]telmisartan to the surface of living RVSMC is saturable and increases quickly to reach equilibrium within 1 h. Telmisartan dissociates very slowly from the receptor with a dissociation half-life (t1/2) of 75 min, which is comparable with candesartan and almost 5 times slower than angiotensin II (AngII). In vivo, telmisartan blunts the blood pressure response to exogenous AngII dose dependently^[1]. Telmisartan (10 mg/kg/d) administration effectively suppresses aneurysm pathogenesis after PPE infusion as well, regardless of whether treatment is initiated before or after aneurysm creation or continues for a limited or extended time. Telmisartan treatment is associated with reduced messenger RNA levels for CCL5 and matrix metalloproteinases 2 and 9 in aneurysmal aortae, with no apparent effect on PPARγ-regulated gene expression^[2]. Telmisartan (1 mg/kg/day) significantly ameliorates neuronal loss and the spatial acquisition impairment in 5XFAD mice, but without any changes of NeuN expression in the hippocampus layer. Telmisartan (1 mg/kg/day) treatment reduces amyloid burden and microglial accumulation in 5XFAD mice brain, induces microglial polarization towards neuroprotective phenotype, but does not alter the expression levels of NEP and IDE in 5XFAD mice specific brain areas^[3]. Telmisartan (0.05, 0.1, 1 mg/kg, p.o.) shows significant reduction in immobility time, antagonizes depression and anxiety, and also significantly attenuates serum cortisol, NO, IL-6 and IL-1β in rats^[4]. Telmisartan (50 μg, i.p.) leads to a 73.2% reduction in tumor growth in mice bearing xenografts derived from OE19 cells. Furthermore, miRNA expression is significantly altered by telmisartan in vivo^[5].

514.62

Solid

C₃₃H₃₀N₄O₂

144701-48-4

替米沙坦

Room temperature in continental US; may vary elsewhere.

DMSO : 6.67 mg/mL(12.96 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 17% Polyethylene glycol 12-hydroxystearate in saline

  Solubility: 3.33 mg/mL (6.47 mM); Suspended solution; Need ultrasonic and warming
• 2.

  请依序添加每种溶剂： 0.5%CMC-Na/saline water

  Solubility: 3 mg/mL (5.83 mM); Suspended solution; Need ultrasonic
• 3.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 0.67 mg/mL (1.30 mM); Clear solution

  此方案可获得 ≥ 0.67 mg/mL (1.30 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 6.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 4.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 0.67 mg/mL (1.30 mM); Clear solution

  此方案可获得 ≥ 0.67 mg/mL (1.30 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 6.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。