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Clevidipine

CAS No. : 167221-71-8

Biological Activity：Clevidipine is a short-acting dihydropyridine calcium channel antagonist (IC50= 7.1 nM, V(H) = -40 mV ) under development for treatment of perioperative hypertension.
IC50 Value: 7.1 nM at V(H) = -40 mV [1]
Target: calcium channel
in vitro: Both clevidipine and nitroglycerin completely reversed U46619-induced contraction (clevidipine (50% effective concentration [EC50] = 3.88 +/- 0.84 x 10(-6) mol/L, nitroglycerin EC50 = 4.84 +/- 2.76 x 10(-8) mol/L) [2]. A decrease in temperature increased the half-life of clevidipine in blood, whereas dilution of the blood did not affect the in vitro half-life of clevidipine. The albumin concentration affected the hydrolysis rate of clevidipine in RBC suspended with saline [3].
in vivo: Clevidipine is a high-clearance drug with a relatively small volume of distribution, resulting in an extremely short half-life in all species studied. The median initial half-life of the individual value (Bayesian estimates) is 12, 20, and 22 s in the rabbit, rat, and dog, respectively [4]. The extremely high clearance value and the small volume of distribution resulted in short half-lives of clevidipine, 2.2 and 16.8 min, respectively. The blood concentration and dose rate producing half the maximal effect (i.e. EC50 and ED50) were approximately 25 nM and 1.5 microg/kg/min, respectively [5].
Clinical trial: CARVE: Clevidipine for Vasoreactivity Evaluation of the Pulmonary Arterial Bed. Phase 4

Research Area：Cardiovascular Disease

Targets：Calcium Channel

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Related Small Molecules:Benidipine hydrochloride;CaV1.3 antagonist-1;14-Deoxyandrographolide;(Rac)-MEM 1003;Glaucine;Efonidipine hydrochloride monoethanolate;L-Ascorbic acid sodium salt;Brompheniramine-d6 maleate;MRS 1523;Nilvadipine;Lercanidipine;CP-060;Anipamil-d25 hydrochloride;ISX-9;ω-Conotoxin MVIIC;Catharanthine;Thapsigargin;Tetrandrine;Ginsenoside Rd;Manidipine dihydrochloride;ω-Agatoxin IVA;AE0047 Hydrochloride;PDE1-IN-4

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