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Phenamil methanesulfonate salt  ≥98%

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包装规格：5mg 25mg in glass bottle
溶解性：溶于DMSO(5mg/mL 加热）
产品描述：基本信息 产品编号： P11305 产品名称： Phenamil methanesulfonate CAS: 1161-94-0   储存条件 粉末 -20℃ 四年 分子式： C12H12ClN7O.CH3SO3H 溶于液体 -80℃(氮气保存) 6个月 分子量： 401.83 -20℃(氮气保存) 1个月 化学名：  3,5-Diamino-6-chloro-N-[imino(phenylamino)methyl]pyrazinecarboxamide methanesulfonate salt Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.4886mL 12.4431mL 24.8861mL 5mM 0.4977mL 2.4886mL 4.9772mL 10mM 0.2489mL 1.2443mL 2.4886mL   生物活性 产品描述 Amiloride的类似物，一种更有效且不可逆的上皮钠通道(ENaC)阻滞剂,一种通过强烈激活BMP信号通路来促进骨修复的小分子。Phenamil methanesulfonate用于囊性纤维化肺疾病的相关研究。 靶点 TRPC3 140nM (IC50)   体外研究 TRPP3,a member of the transient receptor potential (TRP) superfamily of cation channels,is a Ca2+-activated channel permeable to Ca2+,Na+,and K+.TRPP3 is implicated in regulation of pH-sensitive action potential in spinal cord neurons.Phenamil methanesulfonate (1μM) decreases 45Ca2+ uptake in a radiotracer uptake assay.It inhibits TRPP3-mediated Ca2+ transport with an IC50 value of 0.28μM in oocytes expressing TRPP3 or H2O-injected oocytes.Phenamil methanesulfonate is a more potent ENaC blocker than Amiloride,it inhibits the epithelial sodium channel (ENaC) with an IC50 of 400nM (Amiloride=776nM).Phenamil methanesulfonate inhibits basal short-circuit currents with IC50 values of 75 and 116nM,respectively in both human and ovine bronchial epithelia cells.Phenamil methanesulfonate (0-20μM;14 days) elevates adipogenic gene expression,PPARγ,Fabp4,and lipoprotein lipase expression in a concentration-dependent manner,and regulates adipogenesis in C3H10T1/2 cells.Phenamil methanesulfonate (0-20μM;7 or 14 days) modulates MC3T3-E1 osteoblastic differentiation,it increases Alkaline phosphatase (ALP) activity in MC3T3-E1 cells in a concentration-dependent manner. RT-PCR Cell Line: C3H10T1/2 cells Concentration: 0μM and 20μM Incubation Time: 14 days Result: Increased PPARγ,Fabp4,and lipoprotein lipase (LPL) mRNA expression. 体内研究 Phenamil methanesulfonate (subcutaneous injection;15 or 30mg/kg;21 days;infusion rate of 1ml/h) reduces chronichypoxia-induced pulmonary artery hypertension (PAH).Additionally,the mRNA level of SMA,SM22,Id3,and Trb3 from the lung sample are also decreased by Phenamil under hypoxia or normoxia in rats.However,phenamil has little effect on pulmonary vasculature under physiological conditions. Animal Model: Male Sprague-Dawley rats Dosage: 15 or 30mg/kg Administration: Subcutaneous injection;15 or 30mg/kg;21 days;infusion rate of 1ml/h Result:  Reduced hypoxia-induced pulmonary hypertension and vascular remodeling.
保存条件：-20℃

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