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Phenamil methanesulfonate

CAS No. : 1161-94-0

MCE 站：Phenamil methanesulfonate

产品活性：Phenamil methanesulfonate 是 Amiloride (HY-B0285) 的类似物，一种更有效且不可逆的上皮钠通道 (ENaC) 阻滞剂，IC₅₀ 为 400 nM。Phenamil methanesulfonate 也是 TRPP3 的竞争性抑制剂，在 Ca²⁺ 摄取实验中，抑制 TRPP3 介导的 Ca²⁺ 转运的 IC₅₀ 为 140 nM。Phenamil methanesulfonate 是一种通过强烈激活 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。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：Sodium Channel  |  TRP Channel

In Vitro: 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 (1 μM) decreases ⁴⁵Ca²⁺ uptake in a radiotracer uptake assay. It inhibits TRPP3-mediated Ca²⁺ transport with an IC₅₀ value of 0.28 μM 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 400 nM (Amiloride=776 nM).
Phenamil methanesulfonate inhibits basal short-circuit currents with IC₅₀ values of 75 and 116 nM, respectively in both human and ovine bronchial epithelia cells.
Phenamil methanesulfonate (0-20 μM; 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 (0-20 μM; 7 or 14 days) modulates MC3T3-E1 osteoblastic differentiation, it increases Alkaline phosphatase (ALP) activity in MC3T3-E1 cells in a concentration-dependent manner.

In Vivo: Phenamil methanesulfonate (subcutaneous injection; 15 or 30 mg/kg; 21 days; infusion rate of 1 ml/h) reduces chronic-hypoxia-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.

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