A phenylalkylamine L-type calcium channel blocker; blocks recombinant rat L-type calcium channels expressed in tsA201 cells (IC50s = 782 and 8

(±)-Methoxyverapamil (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
16662-46-7
Storage:
-20
UN-No:
Non-Hazardous - /

(±)-Methoxyverapamil is a phenylalkylamine L-type calcium channel blocker and methoxy derivative of verapamil (Item No. 14288).{38991} (±)-Methoxyverapamil blocks recombinant rat L-type calcium channels expressed in tsA201 cells with IC50 values of 782 and 8,000 nM at holding potentials of 10 and -60 mV, respectively. It blocks maitotoxin-induced calcium influx in NIH3T3 fibroblasts (IC50 = 16 μM) and inhibits histamine-induced acid secretion by primary enriched guinea pig parietal cells (IC50 = 10.9 μM).{38992,38993} (±)-Methoxyverapamil binds to rat myocardial membranes (IC50 = 16 nM) and inhibits electrically-stimulated contractions in rat right myocardial ventricular strips (EC50 = 1.95 μM).{38994} In conscious, ovariectomized, post-partum rats, it decreases blood pressure by 30 mm Hg and induces 60% inhibition of uterine contractions when administered at doses of 204 and 324 μg/kg, respectively.{38995}  

 

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Description

A phenylalkylamine L-type calcium channel blocker; blocks recombinant rat L-type calcium channels expressed in tsA201 cells (IC50s = 782 and 8,000 nM at holding potentials of 10 and -60 mV, respectively); blocks maitotoxin-induced calcium influx in NIH3T3 fibroblast cells (IC50 = 16 μM); inhibits histamine-induced acid secretion by primary enriched guinea pig parietal cells (IC50 = 10.9 μM); binds to rat myocardial membranes (IC50 = 16 nM); inhibits electrically-stimulated contractions in rat right myocardial ventricular strips (EC50 = 1.95 μM); decreases blood pressure and inhibits uterine contractions in conscious, ovariectomized, post-partum rats (204 and 324 μg/kg, respectively)

Formal name: α-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-3,4,5-trimethoxy-α-(1-methylethyl)-benzeneacetonitrile, monohydrochloride

Synonyms:  Gallopamil|NSC 274966

Molecular weight: 521.1

CAS: 16662-46-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Cardiovascular System|Heart|Myocardial Contractility||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Endocrinology & Metabolism|Reproductive Biology

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