Clevidipine

Product Details
Formula	C21H23Cl2NO6
Molecular Weight	456.32
Appearance	Solid
Purity	99.88%
Smiles String	O=C(C1=C(C)NC(C)=C(C(OCOC(CCC)=O)=O)C1C2=CC=CC(Cl)=C2Cl)OC

Storage & Handling
Shipping	Room temperature.
Storage	4 °C, protect from light *In solvent : -80 °C, 6 months; -20 °C, 1 month (protect from light)

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 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) . 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 . 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 . 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 . Clinical trial: CARVE: Clevidipine for Vasoreactivity Evaluation of the Pulmonary Arterial Bed. Phase 4

! For research use only. Not intended for any clinical use.