價(jià)格 | ¥239 | ¥339 | ¥578 |
包裝 | 1mg | 2mg | 5mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-09-24 |
中文名稱:LCZ696中間體 | 英文名稱:Sacubitril hemicalcium salt |
CAS:1369773-39-6 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 99.93% | 產(chǎn)品類別: 抑制劑 |
貨號(hào): T4200 |
名稱 | Sacubitril hemicalcium salt |
描述 | Sacubitril hemicalcium salt (AHU377 calcium salt) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696. Sacubitril hemicalcium salt is a prodrug of LBQ657, which is an inhibitor of the zinc metallopeptidase neprilysin. Neprilysin degrades a variety of vasoactive peptides such as atrial and brain natriuretic peptide, bradykinin, adrenomedullin, and endothelin-1. Inhibition of neprilysin leads to an increased level of these peptides and, thus, antihypertensive effects. Formulations containing AHU377 in combination with the angiotensin II receptor antagonist valsartan are used to treat hypertension and heart failure. |
體外活性 | AHU377 is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657. The inactive NEPi precursor, AHU377, does not inhibit collagen accumulation in fibroblasts nor cardiac myocyte hypertrophy. In cardiac fibroblasts, the active NEPi LBQ657 had no discernible effects. In contrast, LBQ657 modestly inhibits cardiac myocyte hypertrophy. |
體內(nèi)活性 | In humans, AHU377 (tmax 0.5-1.1 h) are absorbed quickly. AHU377 is converted rapidly into LBQ657 with its tmax being reached in 1.9-3.5 h. Mean t1/2 values for the biologically active LBQ657 is 9.9-11.1 h.In vehicle-treated dogs, ANF increases urinary sodium excretion from 17.3±3.6 to 199.5±18.4 pequivkglmin. This effect is potentiated significantly in animals which receive AHU377. |
存儲(chǔ)條件 | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 60 mg/mL (69.68 mM) |
關(guān)鍵字 | Cluster of differentiation 10 | Neprilysin | AHU-377 | AHU377 | Sacubitril hemicalcium salt | NEP | inhibit | CD10 | Sacubitril hemicalcium | Sacubitril | Neutral endopeptidase | AHU 377 | AHU-377 hemicalcium | AHU377 calcium | Inhibitor |
相關(guān)產(chǎn)品 | Sacubitril/Valsartan | Sacubitrilat | LHW090-A7 | Thiorphan | Racecadotril | Sacubitril | NEP-IN-1 |
相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 上市藥物庫 | FDA 上市藥物庫 | 抗高血壓化合物庫 | 藥物功能重定位化合物庫 |
成立日期 | 2013-04-18 (12年) | 注冊(cè)資本 | 566.2651萬人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 化學(xué)試劑,生物活性小分子 | 經(jīng)營模式 | 貿(mào)易,試劑,定制,服務(wù) |
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