货号:A120485
同义名:
沙卡布曲 钙盐
/ AHU-377 hemicalcium salt;AHU377 (calcium salt)
Sacubitril hemicalcium salt是一种强效的 Neprilysin 抑制剂,IC50 为 5 nM。
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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免费溶解
描述 | Sacubitril (AHU-377) is a single-molecule drug composed of the molecular parts of Valsartan (ARB) and Sacubitril hemicalsalt (neprilysin inhibitor) (1:1 ratio). Sacubitril (AHU-377) is converted by enzymatic cleavage of ethyl ester to LBQ657, an active metabolite that inhibits neprilysin [2]. Sacubitril hemicalcium salt is an inactive NEPi precursor, which does not inhibit collagen accumulation in fibroblasts nor cardiac myocyte hypertrophy. However, the active NEPi LBQ657 slightly reduces cardiac myocyte hypertrophy without affecting cardiac fibroblasts[3]. |
体内研究 | Sacubitril (AHU-377) demonstrates quick absorption in humans, with a tmax of 0.5-1.1 hours, and its conversion to LBQ657 happens swiftly, reaching its tmax in 1.9-3.5 hours. LBQ657's mean half-life ranges from 9.9 to 11.1 hours[2]. In studies with vehicle-treated dogs, Sacubitril (AHU-377) notably increased urinary sodium excretion and volume following intravenous administration, enhancing the diuretic response to ANF[1]. |
体外研究 | Sacubitril (AHU-377) is a single-molecule drug composed of the molecular parts of Valsartan (ARB) and Sacubitril hemicalsalt (neprilysin inhibitor) (1:1 ratio). Sacubitril (AHU-377) is converted by enzymatic cleavage of ethyl ester to LBQ657, an active metabolite that inhibits neprilysin [2]. Sacubitril hemicalcium salt is an inactive NEPi precursor, which does not inhibit collagen accumulation in fibroblasts nor cardiac myocyte hypertrophy. However, the active NEPi LBQ657 slightly reduces cardiac myocyte hypertrophy without affecting cardiac fibroblasts[3]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.16mL 0.23mL 0.12mL |
5.81mL 1.16mL 0.58mL |
11.61mL 2.32mL 1.16mL |
CAS号 | 1369773-39-6 |
分子式 | C48H56CaN2O10 |
分子量 | 861.044 |
别名 | 沙卡布曲 钙盐 ;AHU-377 hemicalcium salt;AHU377 (calcium salt);Sacubitril |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,Store in freezer, under -20°C |
溶解方案 |
DMSO: 120 mg/mL(139.37 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的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
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动物实验配方 |