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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Endocrinology & Hormones>RAAS inhibitors>Sacubitril
Sacubitril
  • Sacubitril

Sacubitril NEW

Price $57 $77 $116
Package 5mg 10mg 25mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-15

Product Details

Product Name: Sacubitril CAS No.: 149709-62-6
Purity: 98.71% Supply Ability: 10g
Release date: 2024/11/15

Product Introduction

Bioactivity

名稱Sacubitril
描述Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM and is a component of the heart failure medicine LCZ696.
體外活性LCZ696 is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and Sacubitril, a neprilysin inhibitor (1:1 ratio). Sacubitril is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657[2]. The inactive NEPi precursor, Sacubitril, 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[3].
體內(nèi)活性In humans, Sacubitril (tmax0.5-1.1 h) are absorbed quickly. Sacubitril is converted rapidly into LBQ657 with its tmaxbeing reached in 1.9-3.5 h. Mean t1/2values for the biologically active LBQ657 is 9.9-11.1 h[2].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 Sacubitril. Urinary volume is also potentiated in animals which receive an iv administration of Sacubitril[1].
存儲(chǔ)條件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 27.5 mg/mL (66.83 mM)
關(guān)鍵字Neutral endopeptidase | inhibit | Sacubitril | NEP | Neprilysin | antihypertensive | natriuretic peptide | Cluster of differentiation 10 | Inhibitor | COVID-19 | CD10 | heart failure
相關(guān)產(chǎn)品LHW090-A7 | Sacubitril/Valsartan | Racecadotril | NEP-IN-1 | Sacubitril hemicalcium salt | Thiorphan | Sacubitrilat
相關(guān)庫經(jīng)典已知活性庫 | EMA 上市藥物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | FDA 上市藥物庫 | 已知活性化合物庫 | 抗高血壓化合物庫

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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