A TRPP3 inhibitor (IC50 = 140 nM); also inhibits ENaC (IC50 = 400 nM); decreases basal short-circuit currents in human and ovine bronchial epithelial cells (IC50s = 75 and 116 nM

Phenamil (methanesulfonate) – 5 mg

Brand:
Cayman
CAS:
1161-94-0
Storage:
-20
UN-No:
Non-Hazardous - /

Phenamil is an inhibitor of transient receptor potential polycystin-L (TRPP3; IC50 = 140 nM) and a derivative of amiloride (Item No. 14409).{24798} It also inhibits the epithelial sodium channel (ENaC; IC50 = 400 nM).{55255} Phenamil decreases basal short-circuit currents in human and ovine bronchial epithelial cells with IC50 values of 75 and 116 nM, respectively.{24797} It inhibits potassium chloride-induced contractions in isolated rat endothelium-denuded aortic rings (EC50 = 6.76 µM) and increases contractile force in isolated rat right ventricular papillary muscles (EC50 = 16.98 µM).{55253} Phenamil (15 and 30 mg/kg per day) reduces pulmonary artery medial wall thickness and decreases right ventricular peak pressure in a rat model of chronic hypoxia-induced pulmonary hypertension.{55254}  

 

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Description

A TRPP3 inhibitor (IC50 = 140 nM); also inhibits ENaC (IC50 = 400 nM); decreases basal short-circuit currents in human and ovine bronchial epithelial cells (IC50s = 75 and 116 nM, respectively); inhibits potassium chloride-induced contractions in isolated rat endothelium-denuded aortic rings (EC50 = 6.76 µM) and increases contractile force in isolated rat right ventricular papillary muscles (EC50 = 16.98 µM); reduces pulmonary artery medial wall thickness and decreases right ventricular peak pressure in a rat model of chronic hypoxia-induced pulmonary hypertension at 15 and 30 mg/kg per day

Formal name: 3,5-diamino-6-chloro-N-[imino(phenylamino)methyl]-2-pyrazinecarboxamide, monomethanesulfonate

Synonyms: 

Molecular weight: 401.8

CAS: 1161-94-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Immunology & Inflammation|Pulmonary Diseases

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