Aliskiren (CGP 60536; CGP60536B; SPP 100) hydrochloride 是一种口服有效的、选择性的肾素 (renin) 抑制剂，IC50为 1.5 nM。Aliskiren hydrochloride 可用于高血压、心血管疾病和癌症恶病质的研究。

Aliskiren (CGP 60536; CGP60536B; SPP 100) hydrochloride is an orally active and selective renin inhibitor, with IC 50 of 1.5 nM. Aliskiren hydrochloride can be used for the research of hypertension, cardiovascular diseases and cancer cachexia [1] - [4].

Aliskiren hydrochloride inhibits plasma renin activity (PRA) in vitro with IC 50 s of 2.9 nM (human PRA), 8.0 nM (monkey PRA), respectively [1]. Aliskiren hydrochloride (10 μM; 24 h) inhibits prorenin-induced human aortic smooth muscle cell migration [2]. Aliskiren hydrochloride (1-10 μM; 24 h) inhibits both the lamellipodia formation and morphological changes induced by prorenin with no significant effect on PDGF-BB activity [2]. Cell Migration Assay [2] 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 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.

173399-03-6

C30H54ClN3O6

588.22

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years