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173399-03-6

173399-03-6 Structure

173399-03-6 Structure
IdentificationBack Directory
[Name]

(2S,4S,5S,7S)-7-(3-(3-Methoxypropoxy)-4-methoxybenzyl)-5-amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-8-methylnonanamide hydrochloride
[CAS]

173399-03-6
[Synonyms]

Aliskiren HCl
Rasilez Hydrochloride
Tekturna Hydrochloride
Aliskiren Hydrochloride
(2S,4S,5S,7S)-7-(3-(3-Methoxypropoxy)-4-methoxybenzyl)-5-amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-8-methylnonanamide hydrochloride
(αS,γS,δS,zS)-δ-AMino-N-(3-aMino-2,2-diMethyl-3-oxopropyl)-γ-hydroxy-4-Methoxy-3-(3-Methoxypropoxy)-α,z-bis(1-Methylethyl)benzeneoctanaMide Hydrochloride
(2S,4S,5S,7S)-5-AMino-N-(3-aMino-2,2-diMethyl-3-oxopropyl)-4-hydroxy-2-isopropyl-7-(4-Methoxy-3-(3-Methoxypropoxy)benzyl)-8-MethylnonanaMide hydrochloride
[Molecular Formula]

C30H54ClN3O6
[MDL Number]

MFCD13185885
[MOL File]

173399-03-6.mol
[Molecular Weight]

588.23
Chemical PropertiesBack Directory
[Melting point ]

76-78°C
[storage temp. ]

Hygroscopic, -20°C Freezer, Under Inert Atmosphere
[solubility ]

Chloroform, Methanol
[form ]

Solid
[color ]

White to Pale Yellow
[Stability:]

Hygroscopic
Hazard InformationBack Directory
[Chemical Properties]

Off-White Solid
[Uses]

An orally active, synthetic nonpeptide renin inhibitor. Antihypertensive.
[in vivo]

Aliskiren hydrochloride (3 mg/kg, 10 mg/kg; p.o.; daily; 0-12 d) inhibit renin and lower blood pressure without affecting heart rate in sodium-depleted marmosets[3].
Aliskiren hydrochloride (10 mg/kg; p.o.; single dose) delays cachexia development, reduces tumor, and prolongs mouse survival. And also improves whole body strength, mobility and coordination, enhances locomotor activity, and inhibits muscle wasting[4].
Aliskiren hydrochloride (10 mg/kg; p.o.; single dose; 20 d after C26 injection) reduces oxidative stress associated with cancer cachexia[4].

Animal Model:Sodium-depleted marmosets[3]
Dosage:3 mg/kg, 10 mg/kg
Administration:Oral gavage; once daily; 12 days
Result:Increased plasma immunoreactive renin levels, and lowered blood pressure without affecting heart rate.
Showed no rebound increase in BP following the end of treatment with either dose of aliskiren.
Inhibited the RAS and controls the upregulation of pro?inflammatory cytokines.
Animal Model:Cancer cachexia model in BALB/c mice injected with C26 mouse colon carcinoma cells[4]
Dosage:10 mg/kg
Administration:Oral gavage; on day 5 (as a preventive strategy, AP group) or on day 12 (as a therapeutic strategy, AT group) after C26 injection; for 20 days after C26 injection
Result:Enhanced grip strength, coordination, and locomotor activity.
Inhibited serum Ang I and Ⅱ levels and both serum and muscular tumor necrosis factor?α (TNF?α) and inter? leukin?6 (IL?6) levels.
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