Aliskiren hemifumarate

Research use only, not for human use.

The first in a class, potent and highly selective, direct renin inhibitor with IC50 of 0.6 nM.

The first in a class, potent and highly selective, direct renin inhibitor with IC50 of 0.6 nM; no significant inhibition on Cathepsin D, Cathepsin E, Pepsin and HIV-1 peptidase (> 50 uM); orally bioactive.Hypertension Approved(In Vitro):Aliskiren hemifumarate inhibits plasma renin activity (PRA) in vitro with IC50s of 2.9 nM (human PRA), 8.0 nM (monkey PRA), respectively.Aliskiren hemifumarate (5 μM; 24 h) inhibits prorenin-induced human aortic smooth muscle cell migration.Aliskiren hemifumarate (1-10 μM; 24 h) inhibits both the lamellipodia formation and morphological changes induced by prorenin with no significant effect on PDGF-BB activity.(In Vivo):Aliskiren hemifumarate (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.Aliskiren hemifumarate (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.Aliskiren hemifumarate (10 mg/kg; p.o.; single dose; 20 d after C26 injection) reduces oxidative stress associated with cancer cachexia.

Aliskiren hemifumarate inhibits plasma renin activity (PRA) in vitro with IC50s of 2.9 nM (human PRA), 8.0 nM (monkey PRA), respectively.Aliskiren hemifumarate (5 μM; 24 h) inhibits prorenin-induced human aortic smooth muscle cell migration.Aliskiren hemifumarate (1-10 μM; 24 h) inhibits both the lamellipodia formation and morphological changes induced by prorenin with no significant effect on PDGF-BB activity. Cell Viability Assay Cell Line:Smooth muscle cell (SMC) Concentration:1-10 μM Incubation Time:24 hours Result:Inhibited human aortic smooth muscle cell migration induced by prorenin (10 nM) at 10 μM.

Aliskiren hemifumarate (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.Aliskiren hemifumarate (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.Aliskiren hemifumarate (10 mg/kg; p.o.; single dose; 20 d after C26 injection) reduces oxidative stress associated with cancer cachexia. Animal Model:Sodium-depleted marmosets 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 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.

CGP 60536 | CGP60536B | SPP 100

Metabolic Enzyme/Protease

Renin

Renin

Cardiovascular Disease

Hypertension

173334-58-2

1219.589

C64H110N6O16

>98% (HPLC)

10 mM in DMSO

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

Benzeneoctanamide, δ-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-γ-hydroxy-4-methoxy-3-(3-methoxypropoxy)-α,ζ-bis(1-methylethyl)-, (αS,γS,δS,ζS)-, (2E)-2-butenedioate (2:1)

(-20℃)

With Ice Pack

≥ 2 years