Clevidipine Butyrate CAS 167221-71-8

Product Description:

Product Name: Clevidipine butyrate CAS NO: 167221-71-8

Synonyms:

5-O-(butanoyloxymethyl)3-O-methyl4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate;

Cleviprex;

Clevidipine butyrate;

Chemical & Physical Properties:

Appearance: Powder

Assay :≥99.00%

Density: 1.289g/cm3

Boiling Point: 539.7℃ at 760mmHg

Flash Point: 280.2℃

Melting Point: 128-130℃

Storage Temp.: Refrigerator

Vapor Pressure: 0.0±1.4 mmHg at 25℃

Index of Refraction: 1.543

Safety Information:

Safety Statements: S24/25

HS Code: 29339900

Calcium channel blocker, used as an oral antihypertensive.

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 channelin 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

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