Phenamil methanesulfonate|cas:1161-94-0|西域试剂

Phenamil methanesulfonate,98.0%

产品编号：Bellancom-108464A| CAS NO：1161-94-0| 分子式：C₁₃H₁₆ClN₇O₄S| 分子量：401.83

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货号	价格	库存与货期
Bellancom-108464A	￥2000.00	杭州北京（现货）
Bellancom-108464A	￥3350.00	杭州北京（现货）
Bellancom-108464A	￥6000.00	杭州北京（现货）

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Phenamil methanesulfonate

产品介绍

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。

生物活性

Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC₅₀ of 400 nM. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca²⁺ transport with an IC₅₀ of 140 nM in a Ca²⁺ uptake assay. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway^[4]. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease^[5].

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 (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^[4].
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^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR^[4]

Cell Line:	C3H10T1/2 cells
Concentration:	0 μM and 20 μM
Incubation Time:	14 days
Result:	Increased PPARγ, Fabp4, and lipoprotein lipase (LPL) mRNA expression.

体内研究
(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^[5].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley rats^[5]
Dosage:	15 or 30 mg/kg
Administration:	Subcutaneous injection; 15 or 30 mg/kg; 21 days; infusion rate of 1 ml/h
Result:	Reduced hypoxia-induced pulmonary hypertension and vascular remodeling.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley rats^[5]
Dosage:	15 or 30 mg/kg
Administration:	Subcutaneous injection; 15 or 30 mg/kg; 21 days; infusion rate of 1 ml/h
Result:	Reduced hypoxia-induced pulmonary hypertension and vascular remodeling.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley rats^[5]
Dosage:	15 or 30 mg/kg
Administration:	Subcutaneous injection; 15 or 30 mg/kg; 21 days; infusion rate of 1 ml/h
Result:	Reduced hypoxia-induced pulmonary hypertension and vascular remodeling.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (62.22 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4886 mL	12.4431 mL	24.8861 mL
5 mM	0.4977 mL	2.4886 mL	4.9772 mL
10 mM	0.2489 mL	1.2443 mL	2.4886 mL

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.22 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.22 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液