Aliskiren Hemifumarate - CAS 173334-58-2
Catalog number: 173334-58-2
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C30H53N3O6.1/2C4H4O4
Molecular Weight:
1219.61
COA:
Inquire
Targets:
Renin
Description:
Aliskiren hemifumarate is an orally bioactive renin inhibitor (human IC50 = 0.6 nM; rat IC50 = 80 nM) appearing 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. It exhibits an inhibitory activity for arterial vasoconstriction and aldosterone production.
Brife Description:
renin inhibitor, hydrophobic S1/S3-binding pocket
Purity:
>98%
Appearance:
White to Off-White Solid
Synonyms:
Aliskiren fumarate; Aliskiren (hemifumarate); UNII-C8A0P8G029; CHEBI:53777
Solubility:
Soluble in DMSO
MSDS:
Inquire
Shelf Life:
2 years
InChIKey:
KLRSDBSKUSSCGU-KRQUFFFQSA-N
InChI:
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
Canonical SMILES:
CC(C)C(CC1=CC(=C(C=C1)OC)OCCCOC)CC(C(CC(C(C)C)C(=O)NCC(C)(C)C(=O)N)O)N.CC(C)C(CC1=CC(=C(C=C1)OC)OCCCOC)CC(C(CC(C(C)C)C(=O)NCC(C)(C)C(=O)N)O)N.C(=CC(=O)O)C(=O)O
1. Simultaneous Determination of Aliskiren, Amlodipine and Hydrochlorothiazide in Spiked Human Plasma and Urine by High Performance Liquid Chromatography
Zeynep Aydomugs. Journal of Analytical Chemistry, 2015, Vol. 70, No. 4, pp. 502–509.
Aliskiren hemifumarate (Scheme) is the direct rennin enzyme inhibitor clinically used in treatment of hypertension either alone or in combination with other antihypertensive agents. After administration, ALS is rapid ly absorbed with peak plasma concentration occurring after 1–3 h. Its bioavailability is about 2.6% and it is eliminated unchanged primarily by the biliary-fecal route (91%) and renal excretion is only about 0.6%.
2. Ion‑Pair LC Method for Simultaneous Determination of Aliskiren Hemifumarate, Amlodipine Besylate and Hydrochlorothiazide in Pharmaceuticals
Ramzia I. El‑Bagary • Gabor Patonay • Asmaa A. Elzahr • Ehab F. Elkady • Walid A. Ebeid. Chromatographia (2014) 77:257–264
Aliskiren hemifumarate (ALS) (2S,4S,5S,7S)-N-(2-carba-moyl-2-methylpropyl)-5-amino-4-hydroxy-2,7 diisopropyl-8-[4-methoxy-3-(3-methoxypropoxy) phenyl]octanamide hemifumarate) (Fig. 1a), is the first direct renin inhibitor (DRI) suitable for oral administration. By achieving more complete renin–angiotensin system inhibition, direct renin inhibitors may afford greater protection from hypertensive complications. Present evidence indicates that aliskiren reduces baseline systolic and diastolic blood pressure and that it is as effective as other first-line anti-hypertensive agents. Extra advantages can be reached when it is used in combination therapy. Amlodipine besylate (AML) (3-ethyl-5-methyl-(4RS)-2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate benzenesulfonate) (Fig. 1b), is a dihydropyridine long-acting calcium channel blocker that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure. Hydrochlorothiazide is a potent orally diuretic and anti-hypertensive agent which inhibits active chloride reabsorption and thus increases the excretion of sodium chloride and water. It is chemically 6-chloro-1,1-dichloro-3,4-dihydro-2H-1,2,4-benzoliadiazine-7-sulfanomide-1,1-dioxide (Fig. 1c). Triple combination therapy of Aliskiren hemifumarate (ALS), AML and HCZ proved to be effective and well tolerated in treating hypertensive high-risk patients.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Renin Products


CAS 942142-51-0 VTP-27999

VTP-27999
(CAS: 942142-51-0)

VTP-27999 is an alkyl amine Renin inhibitor. It is useful for Hypertension and End-Organ Diseases.

CAS 173334-58-2 Aliskiren Hemifumarate

Aliskiren Hemifumarate
(CAS: 173334-58-2)

Aliskiren hemifumarate is an orally bioactive renin inhibitor (human IC50 = 0.6 nM; rat IC50 = 80 nM) appearing to bind to both the hydrophobic S1/S3-binding po...

CAS 126222-34-2 Remikiren

Remikiren
(CAS: 126222-34-2)

Remikiren is a renin inhibitor originated by Roche in 1996. But clinical trials for the treatment of Heart failure and Hypertension was discontinued.

PD 132002
(CAS: 134452-04-3)

PD 132002 is a renin inhibitor originated by Pfizer. In Dec 2001, clinical trials for Hypertension in USA was discontinued.

CP 84364
(CAS: 114457-62-4)

CP 84364 is an active metabolite of CP-80794 which is a Renin inhibitor.

CAS 1013937-63-7 VTP-27999 2,2,2-trifluoroacetate

VTP-27999 2,2,2-trifluoroacetate
(CAS: 1013937-63-7)

VTP-27999 2,2,2-trifluoroacetate is an alkyl amine Renin inhibitor, useful for Hypertension and End-Organ Diseases.

CAS 1007392-69-9 ACT 178882

ACT 178882
(CAS: 1007392-69-9)

ACT 178882 is a novel Renin inhibitor (IC50= 1.4 nM).

PD 125754
(CAS: 124339-32-8)

This active molecular is a Renin inhibitor that applicated in treatment of essential hypertension.

Chemical Structure

CAS 173334-58-2 Aliskiren Hemifumarate

Quick Inquiry

Verification code

Featured Items