PHENAMIL METHANESULFONATE
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- CAS号:
- 1161-94-0
- 英文名:
- PHENAMIL METHANESULFONATE
- 英文别名:
- MHPIZTURFVSLTJ-UHFFFAOYSA-N;2-Pyrazinecarboxamide, 3,5-diamino-6-chloro-N-[imino(phenylamino)methyl]-, methanesulfonate (1:1)
- 中文名:
- PHENAMIL METHANESULFONATE
- 中文别名:
- 化合物 T23148
- CBNumber:
- CB1502107
- 分子式:
- C13H16ClN7O4S
- 分子量:
- 401.8
- MOL File:
- 1161-94-0.mol
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PHENAMIL METHANESULFONATE化学性质
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储存条件:
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2-8°C
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溶解度:
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45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: soluble2.5mg/mL
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形态:
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solid
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颜色:
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yellow
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CAS 数据库:
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1161-94-0
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PHENAMIL METHANESULFONATE性质、用途与生产工艺
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。
TRPP3, a member of the transient receptor potential (TRP) superfamily of cation channels, is a Ca
2+
-activated channel permeable to Ca
2+
, Na
+
, and K
+
. TRPP3 is implicated in regulation of pH-sensitive action potential in spinal cord neurons.
Phenamil methanesulfonate (1 μM) decreases
45
Ca
2+
uptake in a radiotracer uptake assay. It inhibits TRPP3-mediated Ca
2+
transport with an IC
50
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 IC
50
of 400 nM (Amiloride=776 nM).Phenamil methanesulfonate inhibits basal short-circuit currents with IC
50
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.
RT-PCR
Cell Line:
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C3H10T1/2 cells
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Concentration:
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0 μM and 20 μM
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Incubation Time:
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14 days
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Result:
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Increased PPARγ, Fabp4, and lipoprotein lipase (LPL) mRNA expression.
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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.
Animal Model:
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Male Sprague-Dawley rats
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Dosage:
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15 or 30 mg/kg
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Administration:
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Subcutaneous injection; 15 or 30 mg/kg; 21 days; infusion rate of 1 ml/h
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Result:
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Reduced hypoxia-induced pulmonary hypertension and vascular remodeling.
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PHENAMIL METHANESULFONATE
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1161-94-0, PHENAMIL METHANESULFONATE 相关搜索:
- Amines, Aromatics, Sulfur & Selenium Compounds
- 化合物 T23148
- 1161-94-0
- 2-Pyrazinecarboxamide, 3,5-diamino-6-chloro-N-[imino(phenylamino)methyl]-, methanesulfonate (1:1)
- MHPIZTURFVSLTJ-UHFFFAOYSA-N