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抑制剂描述:

产品名称:LCZ696

产品别名:见爱必信官网

英文别名:LCZ696

靶点:Angiotensin Receptor

CAS:936623-90-4

纯度:≥98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

LCZ696, consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. Phase 3.

溶解性:DMSO : 28 mg/mL (30.6 mM)
Ethanol : 9 mg/mL (9.82 mM), warmed
Water : 92 mg/mL (100.4 mM)

体外研究:

LCZ696 is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and AHU377, a neprilysin inhibitor (1:1 ratio).

体内研究:LCZ696 exerts a blood pressure lowering effect. Blood pressure reduction by LCZ696 is associated with a significant increase in urinary sodium excretion and sympathetic activity suppression. LCZ696 significantly ameliorates cardiac hypertrophy and inflammation, coronary arterial remodeling, and vascular endothelial dysfunction in high-salt loaded SHRcp compared with valsartan. The neprilysin inhibitor component of LCZ696, LBQ657, inhibits hypertrophy but not fibrosis. The angiotensin receptor blocker component of LCZ696, valsartan inhibits both hypertrophy and fibrosis. Dual valsartan+LBQ augment the inhibitory effects of valsartan and the highest doses completely abrogate angiotensin II-mediated effects. Pre-treatment with LCZ696 reduces the ischemic area. The decrease in cerebral blood flow in the peripheral region of the ischemic area is significantly attenuated by pre-treatment with LCZ696. LCZ696 pre-treatment significantly decreases the increase of superoxide anion production in the cortex on the ischemic side.

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