所有图片(1)
别名:
(2S,4S,5S,7S)-N-(2-Carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7diisopropyl-8-[4-methoxy-3-(3-methoxypropoxy)phenyl]-octanamide hemifumarate, CGP-60536, CGP60536B, Rasilez, SPP-100
经验公式（希尔记法）:
C30H53N3O6 · 0.5 C4H4O4
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检测方案
≥95% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
−20°C
SMILES字符串
CC(C)[C@H](C[C@H](N)[C@@H](O)C[C@@H](C(C)C)C(NCC(C)(C)C(N)=O)=O)CC1=CC=C(OC)C(OCCCOC)=C1.OC(/C=C/C(O)=O)=O
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)/b;;2-1+/t2*22-,23-,24-,25-;/m00./s1
InChI key
KLRSDBSKUSSCGU-KRQUFFFQSA-N
生化/生理作用
Aliskiren hemifumarate (ALS) has been used to treat hypertension, alone or with other antihypertensive medications. It is suitable for oral administration. ALS regulates baseline systolic and diastolic blood pressure by blocking the catalytic activity of renin system at its rate-limiting step.
Aliskiren is a potent nonpeptide direct renin inhibitor with an IC50 value of 0.6 nM. It has antihypertensive activity, decreasing plasma renin activity and inhibiting the conversion of angiotensinogen to Angiotensin I by binding to the S3 sub-pocket of renin.
WGK
WGK 3
Jeanette M Wood et al.
Biochemical and biophysical research communications, 308(4), 698-705 (2003-08-21)
Hypertension is a major risk factor for cardiovascular diseases such as stroke, myocardial infarction, and heart failure, the leading causes of death in the Western world. Inhibitors of the renin-angiotensin system (RAS) have proven to be successful treatments for hypertension.
Simultaneous determination of aliskiren hemifumarate, amlodipine besylate, and hydrochlorothiazide in their triple mixture dosage form by capillary zone electrophoresis.
Salim M M, et al.
Journal of Separation Science, 37(9-10), 1206-1213 (2014)
Pharmacovigilance analysis of adverse event reports for aliskiren hemifumarate, a first-in-class direct renin inhibitor.
Ali A K
Therapeutics and Clinical Risk Management, 7, 337-337 (2011)
Chu-Lin Chou et al.
PloS one, 12(7), e0180712-e0180712 (2017-07-13)
Renin-angiotensin system in visceral fat plays a crucial role in the pathogenesis of metabolic syndrome in fructose-fed rats. However, the effects of renin inhibition on visceral adiposity in metabolic syndrome are not fully investigated. We investigated the effects of renin
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