LCZ696中间体|T4200|TargetMol

Sacubitril hemicalcium salt
1369773-39-6

￥239 1mg 起订

￥339 2mg 起订

￥578 5mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: LCZ696中间体

英文名称：: Sacubitril hemicalcium salt

CAS号：: 1369773-39-6

品牌：: TargetMol

产地：: 美国

保存条件：: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.93%

产品类别：: 抑制剂

货号：: T4200

Product Introduction

Bioactivity

名称	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.
体外活性	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.
体内活性	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.
存储条件	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)
关键字	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
相关产品	Phosphoramidon Disodium \| Sacubitril/Valsartan \| Sacubitrilat \| LHW090-A7 \| Thiorphan \| Candoxatril \| Racecadotril \| Sacubitril \| NEP-IN-1
相关库	抑制剂库 \| 经典已知活性库 \| 已知活性化合物库 \| 上市药物库 \| FDA 上市药物库 \| 抗高血压化合物库 \| 药物功能重定位化合物库

LCZ696中间体|||AHU377 calcium salt|||AHU-377 (hemicalcium salt)|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子