Phenamil methanesulfonate

Name: Phenamil methanesulfonate
Brand: MedChemExpress
SKU: HY-108464A
Rating: 4.5 (1 reviews)

Cat. No.: HY-108464A Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease.

For research use only. We do not sell to patients.

Phenamil methanesulfonate Chemical Structure

CAS No. : 1161-94-0

Size	Price	Stock	Quantity
5 mg	USD 85	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 135	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
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100 mg		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of Phenamil methanesulfonate:

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View All Sodium Channel Isoform Specific Products:

View All Isoforms

Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8

View All TRP Channel Isoform Specific Products:

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TRPC TRPM TRPV TRPA TRPML

Biological Activity
Purity & Documentation
References
Customer Review

Description

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)

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].

MedChemExpress (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.

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].

MedChemExpress (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.

Molecular Weight

401.83

Formula

C₁₃H₁₆ClN₇O₄S

CAS No.

1161-94-0

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=NC(Cl)=C(N)N=C1N)NC(NC2=CC=CC=C2)=N.CS(=O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

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

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (62.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (251 KB)

Handling Instructions (2659 KB)

References

[1]. Xiao-Qing Dai , et al. Inhibition of TRPP3 channel by amiloride and analogs. Mol Pharmacol. . 2007 Dec;72(6):1576-85. [Content Brief]

[2]. Andrew J Hirsh, et al.Design, synthesis, and structure-activity relationships of novel 2-substituted pyrazinoylguanidine epithelial sodium channel blockers: drugs for cystic fibrosis and chronic bronchitis. J Med Chem. 2006 Jul 13;49(14):4098-115. [Content Brief]

[3]. Andrew J Hirsh, et al.Evaluation of second generation amiloride analogs as therapy for cystic fibrosis lung disease.J Pharmacol Exp Ther. 2004 Dec;311(3):929-38. [Content Brief]

[4]. Mun Chun Chan, et al. The amiloride derivative phenamil attenuates pulmonary vascular remodeling by activating NFAT and the bone morphogenetic protein signaling pathway. Mol Cell Biol [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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