CAS NO: | 167305-00-2 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Omapatrilat is a dual inhibitor of the metalloproteasesACEandNEPwithKivalues of 0.64 and 0.45 nM, respectively. | ||||||||||||||||
IC50& Target | Ki: 0.45 nM (NEP), 0.64 nM (ACE)[1]; IC50: 8 nM (NEP), 5 nM (ACE)[2] | ||||||||||||||||
体外研究 (In Vitro) | Omapatrilat exhibits high potency for NEP, NEP2 and ACE, moderate strong activity against APP, but low activity against ECE1 (Ki=0.45, 25, 0.64, 250 nM)[1].In vitroautoradiography using the specific NEP inhibitor radioligand 125I-RB104 and the specific ACE inhibitor radioligand 125I-MK351A show omapatril at (10 mg/kg) causes rapid and potent inhibition of renal NEP and ACE, respectively, for 24 h[4]. | ||||||||||||||||
体内研究 (In Vivo) | Omapatrilat demonstrates excellent blood pressure lowering in a variety of animal models characterized by various levels of plasma renin activity and significantly potentiates urinary sodium, ANP, and cGMP excretion in a cynomolgus monkey assay. Omapatrilat decreases mean arterial pressure (MAP) approximately 40 mmHg below baseline from 10 to 24 h. Oral administration of omapatrilat at 100 μM/kg once daily results in a 38 mmHg decrease in systolic blood pressure at day three as compared to vehicle[2]. Omapatrilat is widely used in experimental protocols related to hypertension and heart failure. Chronic oral administration of omapatrilat reduces aortic leakiness and atheroma formation with enhanced endothelial independent vasorelaxation to ANP[3]. Omapatrilat causes significant inhibition of plasma ACE and increased plasma renin activity in rats[4]. | ||||||||||||||||
分子量 | 408.53 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C19H24N2O4S2 | ||||||||||||||||
CAS 号 | 167305-00-2 | ||||||||||||||||
中文名称 | 奥马曲拉 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | -20°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : ≥ 31 mg/mL(75.88 mM) *"≥" means soluble, but saturation unknown. 配制储备液
* 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。 In Vivo: 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
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