Nilvadipine (ARC029) is a potent calcium channel blocker with an IC50 of 0.03 nM. Nilvadipine (ARC029) is used for the treatment of hypertension and chronic major cerebral artery occlusion. Nilvadipine (ARC029) were administrated? intramuscularly in daily doses of 0.01-10 mg/kg for three weeks, starting on the day of cuff-placement. Nilvadipine (ARC029) prvented the cuff-induced intimal thickening in a dose-dependent manner, and was more potent than the other calcium antagonists including nifedipine, diltiazem and verapamil. In an in vitro experiment on inhibition of migration of rat aortic smooth muscle cells, using zymosan-activated air pouch exudate as a chemoattractant in modified Boyden chambers, Nilvadipine (ARC029) was also the most potent among the calcium antagonists tested. The IC50 values were 0.17 nM for nifedipine, 6 nM for verapamil and 0.24 mM for diltiazem. Effects of these drugs on proliferation of rat aortic smooth muscle cells and rabbit platelet aggregation were also examined in vitro. At concentrations less than 10 mM, none of the drugs inhibited proliferation of the smooth muscle cells, and only verapamil inhibited collagen-induced platelet aggregation (IC50 = 0.9 mM).
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 70 mg/mL|
|Related Calcium Channel Products|
|Dantrolene sodium salt
Inhibitor of Ca2+ release from sarcoplasmic reticulum; muscle relaxant.
Thapsigargin is a potent inhibitor of SERCA ATPase.
Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium-channel complexes in the CNS.
Ranolazine is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina.
L-Phenylalanine is an antagonist at α2δ calcium channels with a Ki of 980 nM.
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