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活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
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A409206-1ml |
1ml |
现货 ![]() |
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别名 | 阿利吉仑半富马酸盐 |
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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. 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 lines: Concentrations: Incubation Time: Powder Purity:≥97% |
IC50 | Renin, IC50: 1.5 nM |
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分子类型 | 小分子 |
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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 |
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 |
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Appearance(Colorless Transparent Liquid) | Pass |
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Record the entire process by video | Conform |
Concentration(Compounding value) | 9-11(mmol/L) |