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Phenamil
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Phenamil图片
CAS NO:1161-94-0
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
Phenamil 是 Amiloride 的类似物,是一种更有效且不可逆的上皮钠通道 (ENaC) 阻滞剂,IC50 为 400 nM。
Cas No.1161-94-0
化学名(E)-3,5-diamino-N-(amino(phenylamino)methylene)-6-chloropyrazine-2-carboxamide methanesulfonate
Canonical SMILESClC(N=C1C(/N=C(N)/NC2=CC=CC=C2)=O)=C(N)N=C1N.OS(=O)(C)=O
分子式C12H12ClN7O.CH3SO3H
分子量401.83
溶解度DMF: 0.1 mg/ml,DMSO: 1 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Phenamil is an inhibitor of transient receptor potential polycystin-L (TRPP3; IC50 = 140 nM) and a derivative of amiloride.[1] It also inhibits the epithelial sodium channel (ENaC; IC50 = 400 nM).[2] Phenamil decreases basal short-circuit currents in human and ovine bronchial epithelial cells with IC50 values of 75 and 116 nM, respectively.[3] It inhibits potassium chloride-induced contractions in isolated rat endothelium-denuded aortic rings (EC50 = 6.76 μM) and increases contractile force in isolated rat right ventricular papillary muscles (EC50 = 16.98 μM).[4] Phenamil (15 and 30 mg/kg per day) reduces pulmonary artery medial wall thickness and decreases right ventricular peak pressure in a rat model of chronic hypoxia-induced pulmonary hypertension.[5]

Reference:
[1]. Dai, X.Q., Ramji, A., Liu, Y., et al. Inhibition of TRPP3 channel by amiloride and analogs. Mol. Pharmacol. 72(6), 1576-1585 (2007).
[2]. Hirsh, A.J., Molino, B.F., Zhang, J., et al. Design, synthesis, and structure - activity relationships of novel 2-substituted pyrazinoylguanidine epithelial sodium channel blockers: Drugs for cystic fibrosis and chronic bronchitis. J. Med. Chem. 49(14), 4098-4115 (2006).
[3]. Hirsh, S.J., Sabater, J.R., Zamurs, A., et al. Evaluation of second generation amiloride analogs as therapy for cystic fibrosis lung disease. J. Pharmacol. Exp. Ther. 311(3), 929-938 (2004).
[4]. Brown, L., Cragoe, E.J., Jr., Abel, K.C., et al. Amiloride analogues induce responses in isolated rat cardiovascular tissues by inhibition of Na+/Ca2+ exchange. Naunyn Schmiedebergs Arch Pharmacol. 344(2), 220-224 (1991).
[5]. Chan, M.C., Weisman, A.S., Kang, H., et al. The amiloride derivative phenamil attenuates pulmonary vascular remodeling by activating NFAT and the bone morphogenetic protein signaling pathway. Mol. Cell. Biol. 31(3), 517-530 (2011).