An ENT1 inhibitor (IC50 = 17.5 nM); selective for ENT1 over ENT2 (IC50 = 8

Dilazep (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
20153-98-4
Storage:
-20
UN-No:
Non-Hazardous - /

Dilazep is an inhibitor of equilibrative nucleoside transporter 1 (ENT1; IC50 = 17.5 nM).{49446} It is selective for ENT1 over ENT2 (IC50 = 8,800 nM). Dilazep (0.03 and 0.3 µM) increases adenosine-induced relaxation of, and decreases calcium-induced contractions in isolated guinea pig taenia caeci strips when used at concentrations of 1, 5, and 10 µM.{49447} Dilazep (0.2 mg/kg, i.v.) reduces heart rate and systolic, mean, and diastolic aortic pressure and increases left ventricular blood flow in anesthetized dogs.{49448} It reduces aortic platelet adhesion and aggregation in a rabbit model of aortic injury-induced thrombosis when administered intravenously at a dose of 0.1 mg/kg.{49449}  

 

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Description

An ENT1 inhibitor (IC50 = 17.5 nM); selective for ENT1 over ENT2 (IC50 = 8,800 nM); increases adenosine-induced relaxation of isolated guinea pig taenia caeci strips at 0.03 and 0.3 µM; decreases calcium-induced contractions in isolated guinea pig taenia caeci strips at 1, 5, and 10 µM; reduces heart rate and systolic, mean, and diastolic aortic pressure and increases left ventricular blood flow in anesthetized dogs at 0.2 mg/kg, i.v.; reduces aortic platelet adhesion and aggregation in a rabbit model of aortic injury-induced thrombosis at 0.1 mg/kg

Formal name: 3,4,5-trimethoxy-benzoic acid, 1,1′-[(tetrahydro-1H-1,4-diazepine-1,4(5H)-diyl)di-3,1-propanediyl] ester

Synonyms: 

Molecular weight: 677.6

CAS: 20153-98-4

Purity: ≥98%

Formulation: A solid

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