1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Sodium Channel TRP Channel
  3. Phenamil methanesulfonate

Phenamil methanesulfonate 

目录号: HY-108464A 纯度: ≥98.0%
COA 产品使用指南

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。

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Phenamil methanesulfonate Chemical Structure

Phenamil methanesulfonate Chemical Structure

CAS No. : 1161-94-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[2]. 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[1]. 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].

IC50 & Target[1]

TRPC3

140 nM (IC50)

体外研究
(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[1].
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)[2].
Phenamil methanesulfonate inhibits basal short-circuit currents with IC50 values of 75 and 116 nM, respectively in both human and ovine bronchial epithelia cells[3].
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].

MCE 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].

MCE 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. 
分子量

401.83

Formula

C13H16ClN7O4S

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 25 mg/mL (62.22 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

  • 方案 一

    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); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: ≥98.0%

参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4886 mL 12.4431 mL 24.8861 mL 62.2154 mL
5 mM 0.4977 mL 2.4886 mL 4.9772 mL 12.4431 mL
10 mM 0.2489 mL 1.2443 mL 2.4886 mL 6.2215 mL
15 mM 0.1659 mL 0.8295 mL 1.6591 mL 4.1477 mL
20 mM 0.1244 mL 0.6222 mL 1.2443 mL 3.1108 mL
25 mM 0.0995 mL 0.4977 mL 0.9954 mL 2.4886 mL
30 mM 0.0830 mL 0.4148 mL 0.8295 mL 2.0738 mL
40 mM 0.0622 mL 0.3111 mL 0.6222 mL 1.5554 mL
50 mM 0.0498 mL 0.2489 mL 0.4977 mL 1.2443 mL
60 mM 0.0415 mL 0.2074 mL 0.4148 mL 1.0369 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Phenamil methanesulfonate
目录号:
HY-108464A
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