Phenamil |
Catalog No.GC13994
One-Click Copy Product Info
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Phenamil es un inhibidor selectivo de los canales de potencial transitorio (TRPs) y de los canales iónicos sensibles al ácido (ASICs).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1161-94-0
Sample solution is provided at 25 µL, 10mM.
Phenamil es un inhibidor selectivo de los canales de potencial transitorio (TRPs) y de los canales iónicos sensibles al ácido (ASICs) [1]. Phenamil es un análogo de la amilorida y un bloqueador más potente y menos reversible del canal de sodio epitelial (ENaC) con un IC50 de 400 nM [2]. Phenamil inhibió el transporte de Ca2+ mediado por TRPP3 con un IC50 de 140 nM en un ensayo de captación de Ca2+ [3].
El tratamiento con Phenamil (10 µM) de células madre mesenquimales (MSC) de ratón M2-10B4 (M2) durante 6 días con 10 µM de phenamil estimuló notablemente la expresión de los genes que codifican ALP, Runx2, OCN y osterix. Phenamil induce la expresión de genes osteogénicos y la mineralización tanto en cultivos de MSC como en cultivos de órganos primarios de calvaria [4]. Phenamil (10 µM) indujo la expresión de PPARγ dentro de las 24 h en líneas celulares preadipocíticas 3T3-F442A. Phenamil actúa como un nuevo compuesto proadipogénico [5].
Phenamil (15 o 30 mg/kg; 21 días) redujo la hipertensión arterial pulmonar (HAP) inducida por hipoxia crónica. La infusión de phenamil durante el tratamiento de hipoxia inhibió la remodelación vascular pulmonar [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.
| Experimentos celulares [1]: | |
Líneas celulares | Células osteoblásticas tipo MC3T3-E1 |
Método de preparación | Las células se mantuvieron en un medio de cultivo regular, es decir, α-mínimo medio esencial suplementado con 10% de suero fetal bovino (FBS), 100 U/ml de penicilina G y 100 mg/ml de estreptomicina. El medio de cultivo, con o sin 10 µM de fenamil, se reemplazó cada 3-4 días. |
Condiciones de reacción | 10 µM durante 14 días |
Áreas de aplicación | Las células tratadas con fenamil y las células control no tratadas mostraron un aumento estadísticamente significativo en la proliferación celular desde el día 7 hasta el día 14. |
| Experimentos con animales [2]: | |
Modelos animales | Ratas Sprague-Dawley machos |
Método de preparación | Se implantaron bombas de infusión osmótica en miniatura que administran una solución de salina-DMSO (50% salina-50% DMSO) o fenamil en salina-DMSO subcutáneamente en ratas Sprague-Dawley machos (edad, 6 a 7 semanas; peso, 250 a 300 g) entre las escápulas y conectadas a través de un catéter avanzado en la arteria carótida izquierda. Se utilizaron cuatro ratas para cada condición. El fenamil (15 o 30 mg/kg de peso corporal/día) se administró de manera continua durante 21 días a una velocidad de infusión de 1 ml/h. Las ratas fueron sometidas a hipoxia hipobárica (10.5% de oxígeno) o normoxia (aire ambiente) durante 21 días. |
Forma de dosificación | 15 o 30 mg/kg, bomba de infusión osmótica en miniatura |
Áreas de aplicación | El fenamil reduce la hipertensión arterial pulmonar (HAP) inducida por hipoxia crónica. |
Referencias: [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] 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. | |
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4886 mL | 12.4431 mL | 24.8861 mL |
| 5 mM | 497.7 μL | 2.4886 mL | 4.9772 mL |
| 10 mM | 248.9 μL | 1.2443 mL | 2.4886 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)