坎地沙坦酯 T2400

Product Introduction
Bioactivity


英文名: Candesartan Cilexetil

描述: Candesartan Cilexetil (TCV-116) 是一种血管紧张素II 拮抗剂，可用于治疗高血压。

激酶实验: Kinetic Methods: In a typical kinetic run, 2.00 mL of assay buffer (20 mM HEPES, 0.5 mM EDTA, 0.035% SDS, pH 7.8) and Suc-Leu-Leu-Val-Tyr-AMC in DMSO are added to a 3 mL fluorescence cuvette, and the cuvette is placed in the jacketed cell holder of a fluorescence spectrophotometer. Reaction temperature is maintained at 37℃ by a circulating water bath. After the reaction solution has reached thermal equilibrium (5 minutes), 1 μL?10 μL of the stock enzyme solution is added to the cuvette. Reaction progress is monitored by the increase in fluorescence emission at 440 nm (λex= 380 nm) that accompanies cleavage of AMC from peptide-AMC substrates.

体外活性: 给药5小时后,Candesartan（1 mg/kg,p.o.）在第1和第7天,与依那普利（10 mg/kg,p.o.）以相同的程度降低血压.Candesartan使肾血流量显著增加,但心脏指数无变化.在DCM大鼠的心肌中,Candesartan剂量依赖性地提高功能标记并上调血管紧张素（1-7）,ACE2和MAS1.在Candesartan处理的大鼠中,Candesartan使各种ER应激、凋亡标志物及凋亡细胞的数目降低.在扩张型心肌病的大鼠中,Candesartan剂量依赖性地显示对血管紧张素-II的阻断作用.

体内活性: Candesartan的前药经胃肠道吸收酯水解活化为Candesartan。Candesartan阻断血管紧张素II对血管紧张素II类型1受体的影响。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 61.1 mg/mL (100 mM)


关键字: inhibit | Angiotensin Receptor | Apoptosis | Inhibitor | TCV116 | Candesartan Cilexetil | TCV 116

相关产品: Ethyl pyruvate | Taurolidine | Flurochloridone | Irbesartan | ROC-325 | Desoxyrhaponticin | MAZ51 | Escin | XX-650-23 | SZL P1-41

相关库: Drug Repurposing Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Human Metabolite Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | Orally Active Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途