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Aliskiren Hemifumarate(CGP 60536)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Aliskiren Hemifumarate(CGP 60536)图片
CAS NO:173334-58-2
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)609.83
FormulaC30H53N3O6.1/2C4H4O4
CAS No.173334-58-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (164.0 mM)
Water: 100 mg/mL (164.0 mM)
Ethanol: 100 mg/mL (164.0 mM)
Other info

Chemical Name: (αS,γS,δS,ζS)-δ-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-γ-hydroxy-4-methoxy-3-(3-methoxypropoxy)-α,ζ-bis(1-methylethyl)-benzeneoctanamide, 2E-butenedioate

InChi Key: KLRSDBSKUSSCGU-KRQUFFFQSA-N

InChi Code: InChI=1S/2C30H53N3O6.C4H4O4/c2*1-19(2)22(14-21-10-11-26(38-8)27(15-21)39-13-9-12-37-7)16-24(31)25(34)17-23(20(3)4)28(35)33-18-30(5,6)29(32)36;5-3(6)1-2-4(7)8/h2*10-11,15,19-20,22-25,34H,9,12-14,16-18,31H2,1-8H3,(H2,32,36)(H,33,35);1-2H,(H,5,6)(H,7,8)

SMILES Code: COC1=C(OCCCOC)C=C(C[C@H](C(C)C)C[C@H](N)[C@@H](O)C[C@H](C(NCC(C)(C)C(N)=O)=O)C(C)C)C=C1.OC(/C=C/C(O)=O)=O

Synonyms

CGP060536B; SPP-100; CGP 060536B; SPP 100; CGP-060536B; Rasilez; SPP100; Tekturna

实验参考方法
In Vitro

In vitro activity: 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 VivoAliskiren 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.
Animal model
Formulation & Dosage< 10 mg/kg, oral
References

Pharmacol Rep. 2008 Sep-Oct;60(5):623-31; Biochem Biophys Res Commun. 2003 Sep 5;308(4):698-705.