Aliskiren Hemifumarate, 肾素抑制剂

肾素选择性抑制剂
  • 10mM in DMSO
有货

库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
A409206-1ml
1ml 现货 Stock Image
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Compound libraries (12332)

基本描述

别名 阿利吉仑半富马酸盐
英文别名 (2S,4S,5S,7S)-7-(4-methoxy-3-(3-methoxypropoxy)benzyl)-5-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-2-isopropyl-8-methylnonanamide hemifumarate
规格或纯度 10mM in DMSO
英文名称 Aliskiren Hemifumarate
生化机理 阿利吉仑半富马酸盐是一种直接肾素抑制剂,IC50 为 1.5 nM。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 肾素抑制剂
产品介绍

Aliskiren Hemifumarate是一种直接肾素抑制剂,IC50为1.5 nM。

Information

Aliskiren hemifumarate is a directrenininhibitor withIC50of 1.5 nM.
In vitro

Aliskiren hemifumarate appears to bind to both the hydrophobic S1/S3-binding pocket and to a large, distinct subpocket that extends from the S3-binding site towards the hydrophobic core of renin. Oral bioavailability of Aliskiren hemifumarate is 2.4% in rats, 16% in marmosets and about 2.5% in humans.

In vivo

Aliskiren hemifumarate (< 10 mg/kg, oral) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets. Once-daily oral treatment with Aliskiren hemifumarate lowers blood pressure effectively, with a safety and tolerability profile, in patients with mild-to-moderate hypertension.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥97%

产品属性

IC50 Renin, IC50: 1.5 nM

关联靶点(人)

REN Tclin 肾素(Renin) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES COCCCOC1=C(OC)C=CC(=C1)CC(CC(N)C(O)CC(C(C)C)C(=O)NCC(C)(C)C(N)=O)C(C)C.COCCCOC2=C(OC)C=CC(=C2)CC(CC(N)C(O)CC(C(C)C)C(=O)NCC(C)(C)C(N)=O)C(C)C.OC(=O)\C=C\C(O)=O
分子量 609.83

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 85 mg/mL (200.74 mM); Water: 85 mg/mL (200.74 mM); Ethanol: 8 mg/mL

安全和危险性(GHS)

技术规格说明书

Appearance(Colorless Transparent Liquid) Pass
Record the entire process by video Conform
Concentration(Compounding value) 9-11(mmol/L)

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

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