Phenamil methanesulfonate

Name: Phenamil methanesulfonate
Brand: TargetMol
SKU: T23148
Rating: 4.5 (1 reviews)

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Catalog No. T23148Cas No. 1161-94-0

Phenamil methanesulfonate is a potent analog of Amiloride that functions as a strong and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM, Phenamil methanesulfonate also acts as a competitive inhibitor of TRPP3 and suppressing TRPP3-mediated calcium transport with an IC50 of 140 nM in Ca2+ uptake assays. Phenamil methanesulfonate robustly activates BMP signaling to promote bone repair, supporting its use in cystic fibrosis lung disease, ion channel biology, and regenerative medicine research.

Phenamil methanesulfonate

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Catalog No. T23148Cas No. 1161-94-0

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Product Introduction

Bioactivity

Description	Phenamil methanesulfonate is a potent analog of Amiloride that functions as a strong and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM, Phenamil methanesulfonate also acts as a competitive inhibitor of TRPP3 and suppressing TRPP3-mediated calcium transport with an IC50 of 140 nM in Ca2+ uptake assays. Phenamil methanesulfonate robustly activates BMP signaling to promote bone repair, supporting its use in cystic fibrosis lung disease, ion channel biology, and regenerative medicine research.
Targets&IC50	ENaC:400 nM
In vitro	Beyond channel blockade, in C3H10T1/2 mesenchymal cells, Phenamil methanesulfonate regulated adipogenesis in a concentration-dependent manner (0-20 μM) by elevating the expression of adipogenic genes such as PPARγ and Fabp4 [4]. Additionally, in MC3T3-E1 osteoblastic cells, it promoted osteoblastic differentiation, evidenced by a concentration-dependent increase in Alkaline Phosphatase (ALP) activity [4].
In vivo	In a rat model of chronic-hypoxia-induced pulmonary artery hypertension (PAH), Phenamil methanesulfonate demonstrated significant therapeutic efficacy. Administration via continuous subcutaneous infusion (15 or 30 mg/kg/day) for 21 days effectively reduced the severity of PAH. Mechanistically, the compound downregulated the mRNA expression of smooth muscle markers in lung tissues [4].

Chemical Properties

Molecular Weight	401.83
Formula	C₁₃H₁₆ClN₇O₄S
Cas No.	1161-94-0
Smiles	O=C(NC(=N)NC=1C=CC=CC1)C2=NC(Cl)=C(N=C2N)N.O=S(=O)(O)C
Relative Density.	1.31g/cm3

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 20 mg/mL (49.77 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4886 mL	12.4431 mL	24.8861 mL	124.4307 mL
5 mM	0.4977 mL	2.4886 mL	4.9772 mL	24.8861 mL
10 mM	0.2489 mL	1.2443 mL	2.4886 mL	12.4431 mL
20 mM	0.1244 mL	0.6222 mL	1.2443 mL	6.2215 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc