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BUY Azelnidipine

BUY Azelnidipine

Cat no: A-135


Supplier: Alomone Labs Limited.
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Both L-type (CaV1) and T-type (CaV3) voltage gated Ca2+ channels are large (~0.5 MDa), transmembrane proteins which control the cellular influx of Ca2+ in response to electrical stimulus; while CaV1s require a strong depolarization (~+40 mV) to perform, a much weaker pulse (~-40 mV) is sufficient to activate CaV3s. Ca2+ channel blockers (CCBs) are a diverse class of pharmaceutical agents, usually targeting L-type channels, of which dihydropyridines (DHPs) constitute a major subgroup. Inhibitors of Ca2+-mediated smooth muscle contractions, CCBs produce vasodilation, thus therapeutically managing hypertension and coronary heart disease. An antagonist of both CaV1 (all subtypes) and CaV3 ((A)1G and (A)1H subtypes), azelnidipine (AZL) is a DHP derivate known to target CaVs with an IC50 of 3 nM. Its long-lasting interaction at multiple binding sites of L-type Ca2+ channels renders it resistant to S(-)-Bay K 8644 (CaV1 channel agonist) activating effects, otherwise shown to counteract nifedipine-induced inhibition; AZL thus confers significantly prolonged cardioactive time. Its reduced side effects and improved cardiovagal baroreflex sensitivity (BRS) when clinically administered make ALZ's therapeutic benefits superior to that of the potent antihypertensive, amlodipine. Additionally, ALZ possesses hydragogue, heart-protective, kidney-protective, and anti-arteriosclerosis capabilities.
Catalogue number: A-135
Size: 25 mg
Concentration: 1-100 uM
Molecular weight: 582.65 Da
Purity: >98%
Shipping temp: Room Temperature