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| 品牌 | absin | CAS | 1369773-39-6 |
|---|---|---|---|
| 分子式 | C24H28Ca0.5NO5 | 纯度 | ＞98% |
| 分子量 | 430.52 | 货号 | abs814191 |
| 规格 | 50mg | 供货周期 | 现货 |
| 主要用途 | is an inhibitor of neprilysin with IC50 | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
AHU-377 hemicalcium salt 1369773-39-6
| 产品描述 | |
| 描述 | AHU-377 is an inhibitor of neprilysin with IC50 value of 5 nM. |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | AHU-377,AHU 377 ,AHU377 |
| 外观 | Powder |
| 可溶性/溶解性 | DMSO: ≥ 54 mg/mL |
| 生物活性 | |
| 靶点 | Neprilysin |
| In vitro(体外研究) | LCZ696 is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and AHU377, a neprilysin inhibitor (1:1 ratio). 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. |
| In vivo(体内研究) | 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±18.4pequivkglmin. This effect is potentiated significantly in animals which receive AHU377. Urinary volume is also potentiated in animals which receive an iv administration of AHU377. |
| 参考文献 | |
| 参考文献 | [1]. Schiering N,et al. Structure of neprilysin in complex with the active metabolite of sacubitril.Sci Rep. 2016 Jun 15;6:27909. |
| 研究领域 | |
| 研究领域 | Signal TransductionMetabolism Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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