Aliskiren Hemifumarate - 10mM in DMSO , Renin inhibitor, CAS No.173334-58-2, Renin inhibitor

CAS: 173334-58-2 Cat. No.: A409206 Peso molecular: 609.83 Número EC: 630-415-8 PubChem CID: 6918427

GRADE & PURITY 10mM in DMSO

Synonyms

(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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Aliskiren hemifumarate is a directrenininhibitor withIC50of 1.5 nM.
In vitro

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 Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥97%

Specifications

Sinónimos

(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

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Aliskiren hemifumarate is a direct renin inhibitor with IC50 of 1.5 nM.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

INHIBITOR

Mecanismo de acción

Renin inhibitor

Nombres e identificadores

• Isómeros SMILES: CC(C)[C@@H](CC1=CC(=C(C=C1)OC)OCCCOC)C[C@@H]([C@H](C[C@@H](C(C)C)C(=O)NCC(C)(C)C(=O)N)O)N.CC(C)[C@@H](CC1=CC(=C(C=C1)OC)OCCCOC)C[C@@H]([C@H](C[C@@H](C(C)C)C(=O)NCC(C)(C)C(=O)N)O)N.C(=C/C(=O)O)\C(=O)O
• PubChem CID: 6918427
• Peso molecular: 609.83

Objetivos asociados (humanos)

REN Tclin Renin (2 Activities)

Discover Target: REN

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 85 mg/mL (200.74 mM); Water: 85 mg/mL (200.74 mM); Ethanol: 8 mg/mL