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Phenamil

Catalog No.GC13994

Phenamil, an analog of Amiloride, is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM.

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Phenamil Chemical Structure

Cas No.: 1161-94-0

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5mg
$84.00
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10mg
$117.00
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50mg
$490.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Osteoblast-like MC3T3-E1 cells

Preparation Method

The cells were maintained in regular growth medium, i.e. α-minimal essential medium supplemented with 10% fetal bovine serum (FBS), 100 U/ml penicillin G and 100 mg/ml streptomycin. The culture medium, with or without 10 µM phenamil, was replaced every 3-4 days.

Reaction Conditions

10 µM for 14 days

Applications

Phenamil-treated and -untreated control cells showed a statistically significant increase in cell proliferation from day 7 to day 14.

Animal experiment [2]:

Animal models

Male Sprague-Dawley rats

Preparation Method

Miniature osmotic infusion pumps which deliver saline-DMSO (50% saline-50% DMSO) solution or phenamil in saline-DMSO were implanted subcutaneously in male Sprague-Dawley rats (age, 6 to 7 weeks; weight, 250 to 300 g) between the scapulae and connected via a catheter advanced into the left carotid artery. Four rats were used for each condition. Phenamil (15 or 30 mg/kg of body weight/day) was administered continuously for 21 days at an infusion rate of 1 ml/h. The rats were subjected to hypobaric hypoxia (10.5% oxygen) or normoxia (room air) for 21 days.

Dosage form

15 or 30 mg/kg, Miniature osmotic infusion pump

Applications

Phenamil reduces chronic-hypoxia-induced pulmonary artery hypertension (PAH).

References:

[1] : Lo K W H, Ulery B D, Kan H M, et al. Evaluating the feasibility of utilizing the small molecule phenamil as a novel biofactor for bone regenerative engineering[J]. Journal of tissue engineering and regenerative medicine, 2014, 8(9): 728-736.

[2] :Chan M C, Weisman A S, Kang H, et al. The amiloride derivative phenamil attenuates pulmonary vascular remodeling by activating NFAT and the bone morphogenetic protein signaling pathway[J]. Molecular and cellular biology, 2011, 31(3): 517-530.

Background

Phenamil is a selective inhibitor of transient receptor potentials (TRPs) and acid-sensing ion channels (ASICs) [1]. Phenamil is an amiloride analogs and a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM [2]. Phenamil inhibited TRPP3 -mediated Ca2+ transport with an IC50 of 140 nM in a Ca2+ uptake assay [3].

Phenamil (10 µM) Treatment of M2-10B4 (M2) mouse (mesenchymal stem cells) MSCs for 6 days with 10 µM phenamil markedly stimulated expression of the genes encoding ALP, Runx2, OCN, and osterix. Phenamil induces osteogenic gene expression and mineralization in both MSC and primary calvariae organ cultures [4]. Phenamil (10 µM) induced the expression of PPARγ within 24 h in 3T3-F442A preadipocyte cell lines. Phenamil act as a new proadipogenic compound [5].

Phenamil (15 or 30 mg/kg; 21 days) reduced chronic-hypoxia-induced pulmonary artery hypertension (PAH). Infusion of phenamil during hypoxia treatment inhibited pulmonary vascular remodeling [6].

References:
[1]. Chan M C, Weisman A S, Kang H, et al. The amiloride derivative phenamil attenuates pulmonary vascular remodeling by activating NFAT and the bone morphogenetic protein signaling pathway[J]. Molecular and cellular biology, 2011, 31(3): 517-530.
[2]. Hirsh A J, Molino B F, Zhang J, 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]. Journal of medicinal chemistry, 2006, 49(14): 4098-4115.
[3]. Dai X Q, Ramji A, Liu Y, et al. Inhibition of TRPP3 channel by amiloride and analogs[J]. Molecular pharmacology, 2007, 72(6): 1576-1585.
[4]. Park K W, Waki H, Kim W K, et al. The small molecule phenamil induces osteoblast differentiation and mineralization[J]. Molecular and cellular biology, 2009, 29(14): 3905-3914.
[5]. Park K W, Waki H, Choi S P, et al. The small molecule phenamil is a modulator of adipocyte differentiation and PPARγ expression [S][J]. Journal of lipid research, 2010, 51(9): 2775-2784.
[6]. Chan M C, Weisman A S, Kang H, et al. The amiloride derivative phenamil attenuates pulmonary vascular remodeling by activating NFAT and the bone morphogenetic protein signaling pathway[J]. Molecular and cellular biology, 2011, 31(3): 517-530.

Chemical Properties

Cas No. 1161-94-0 SDF
Chemical Name (E)-3,5-diamino-N-(amino(phenylamino)methylene)-6-chloropyrazine-2-carboxamide methanesulfonate
Canonical SMILES ClC(N=C1C(/N=C(N)/NC2=CC=CC=C2)=O)=C(N)N=C1N.OS(=O)(C)=O
Formula C12H12ClN7O.CH3SO3H M.Wt 401.83
Solubility DMF: 0.1 mg/ml,DMSO: 1 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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