替莫普利 T20689

Product Introduction
Bioactivity


英文名: Temocaprilat

描述: Temocaprilat (RS5139) 是一种血管紧张素转换酶 (ACE) 抑制剂。 Temocaprilat 通过缺乏 EHBR 的 cMOAT 有效地从胆汁中排泄，而许多其他 ACE 抑制剂对 cMOAT 的亲和力较低。

体内活性: Biliary clearance of Temocaprilat after i.v. administration of [14C]temocapril x HCl (1.0 mg/kg) in EHBR was significantly lower than that in Sprague-Dawley rats (5.00 ml/min/kg for Sprague-Dawley rats vs. 0.25 ml/min/kg for EHBR). The uptake of Temocaprilat into canalicular membrane vesicles (CMVs) prepared from Sprague-Dawley rats was stimulated in the presence of ATP, whereas little stimulation was observed in CMVs from EHBR. The initial uptake rate of ATP-dependent transport of Temocaprilat showed saturation kinetics; we obtained an apparent V(max) value of 1.14 nmol/min/mg protein and a K(m) value 92.5 microM. ATP-dependent transport of Temocaprilat was competitively inhibited by 2,4-dinitrophenyl-S-glutathione, a typical substrate for cMOAT with an inhibition constant (K(i)) of 25.8 microM. The K(m) value for the uptake of 2,4-dinitrophenyl-S-glutathione into CMVs (K(m) = 29.6 microM) was consistent with this K(i) value. In addition, the ATP-dependent uptake of 2,4-dinitrophenyl-S-glutathione was inhibited by Temocaprilat in a concentration-dependent manner. Active forms of some ACE inhibitors (benazepril, cilazapril, delapril, enalapril and imidapril) did not affect the transport of Temocaprilat into CMVs even at concentrations as high as 200 microM[1].

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

溶解度: DMSO : 4.49 mg/mL (10 mM)


关键字: Temocaprilat

相关产品: L-Isoleucyl-L-arginine | Rentiapril racemate | Zabicipril HCl | Palatrigine | Garcinone B | Tuna AI acetate | Ovalbumin (154-159) | Libenzapril | Isocrenatoside | Trandolapril

相关库: Bioactive Compounds Library Max | Human Metabolite Library | Inhibitor Library | Metabolism Compound Library | Bioactive 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