產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 10mg 50mg 100mg
CAS	159138-80-4
別名
化學名	(Z)-N-carbamimidoyl-4-isopropyl-3-(methylsulfonyl)benzimidic acid
分子式	C12H17N3O3S
分子量	283.35
溶解度	≥ 12.05mg/mL in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Description:

IC50: 0.05, 3 and 1000 μM for NHE1, NHE3 and NHE2, respectively

Na–H exchange (NHE) represents an important mechanism for mediating such injury. NHE represents an important mechanism for the development of myocardial ischemic and reperfusion injury and inhibitors have been consistently shown to protect the ischemic and reperfused heart by correcting the ionic imbalance associated with this form of pathological insult. Cariporide is a potent NHE inhibitor.

In vitro: Cariporide concentration dependently inhibited the amiloride sensitive sodium influx in rabbit erythrocytes, reduced the swelling of human platelets caused by intracellular acidification, and delayed pH recovery in rat cardiomyocytes [1].

In vivo: In anaesthetised rats undergoing coronary artery ligation intravenous and oral pretreatment with Cariporide caused a dose dependent reduction or a complete prevention of ventricular premature beats, ventricular fibrillation, and ventricular tachycardia. The compound was well tolerated and neutral to circulatory variables [1].

Clinical trial: Cariporide has been evaluated in a large dose-finding Phase II/Phase III clinical trial to assess the efficacy in patients with acute coronary syndromes. Overall results failed to demonstrate protection but sub-group analysis revealed significant risk reductions with the highest cariporide dose especially in high risk patients undergoing coronary artery bypass surgery [2].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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