| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
TRPC3 140 nM (IC50)
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| ln Vitro |
TRPP3, a cation channel that belongs to the transient receptor potential (TRP) superfamily, is triggered by Ca2+ and permeable to Ca2+, Na+, and K+. In spinal cord neurons, TRPP3 is involved in the control of pH-sensitive action potentials. In radiotracer uptake experiment, phenamil methanesulfonate (1 μM) reduces 45Ca2+ absorption. With an IC50 value of 0.28 μM in oocytes expressing TRPP3 or oocytes injected with H2O, it inhibits TRPP3-mediated Ca2+ transport[1]. The epithelial sodium channel (ENaC) is inhibited by phenamil methanesulfonate, a more powerful ENaC blocker than amiloride, with an IC50 of 400 nM (vs 776 nM for amiloride)[2]. In both human and ovine bronchial epithelia cells, phenolmethyl methanesulfonate suppresses baseline short-circuit currents with IC50 values of 75 and 116 nM, respectively[3]. In C3H10T1/2 cells, phenamil methanesulfonate (0–20 μM; 14 days) controls adipogenesis and increases the expression of PPARγ, Fabp4, lipoprotein lipase, and adipogenic genes in a concentration-dependent manner[4]. Methanesulfonate (0–20 μM; 7 or 14 days) boosts concentration-dependently the activity of alkaline phosphatase (ALP) in MC3T3–E1 cells and modifies their osteoblastic differentiation[4].
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| ln Vivo |
PAH caused by chronic hypoxia is lessened by phenamil methanesulfonate (subcutaneous injection; 15 or 30 mg/kg; 21 days; infusion rate of 1 ml/h). Furthermore, Phenamil reduces the mRNA levels of SMA, SM22, Id3, and Trb3 in the lung sample in rats under hypoxia or normoxia. Phenamil, however, has minimal effects on the pulmonary vasculature in a physiological setting[5].
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| Cell Assay |
RT-PCR[4]
Cell Types: C3H10T1/2 cells Tested Concentrations: 0 μM and 20 μM Incubation Duration: 14 days Experimental Results: Increased PPARγ, Fabp4, and lipoprotein lipase (LPL) mRNA expression. |
| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats[5]
Doses: 15 or 30 mg /kg Route of Administration: subcutaneous (sc) injection; 15 or 30 mg/kg; 21 days; infusion rate of 1 ml/h Experimental Results: decreased hypoxia-induced pulmonary hypertension and vascular remodeling. |
| References |
[1]. Xiao-Qing Dai , et al. Inhibition of TRPP3 channel by amiloride and analogs. Mol Pharmacol. . 2007 Dec;72(6):1576-85.
[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. [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. [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 |
| Molecular Formula |
C13H16CLN7O4S
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|---|---|
| Molecular Weight |
401.83
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| CAS # |
1161-94-0
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| SMILES |
N=C(NC(C1=NC(Cl)=C(N=C1N)N)=O)NC2=CC=CC=C2.CS(=O)(O)=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25 mg/mL (62.22 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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