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SML2077

Sigma-Aldrich

Aliskiren hemifumarate

≥95% (HPLC)

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

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About This Item

经验公式（希尔记法）:
C30H53N3O6 · 0.5 C4H4O4
CAS号:
173334-58-2
分子量:
609.79
MDL编号:
MFCD27756642
UNSPSC代码:
12352200
NACRES:
NA.77

方案

≥95% (HPLC)

表单

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.
Direct renin inhibitor; anti-hypertensive

储存分类代码

11 - Combustible Solids

WGK

WGK 3

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000350493
0000350493
0000132386
0000132386
0000132385

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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.
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)
Nikolaos-Dimitrios Pantzaris et al.
Journal of clinical medicine, 6(6) (2017-06-10)
The renin-angiotensin-aldosterone system (RAAS) plays a key role in the pathophysiology of arterial hypertension as well as in more complex mechanisms of cardiovascular and renal diseases. RAAS-blocking agents like angiotensin-converting enzyme (ACE) inhibitors and angiotensin II receptor blockers, have long
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)
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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