1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. Calcium Channel
  3. Clevidipine

Clevidipine 

Cat. No.: HY-17436 Purity: 99.69%
Handling Instructions

Clevidipine is a short-acting dihydropyridine calcium channel antagonist (IC50= 7.1 nM, V(H) = -40 mV ) under development for treatment of perioperative hypertension.

For research use only. We do not sell to patients.

Clevidipine Chemical Structure

Clevidipine Chemical Structure

CAS No. : 167221-71-8

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Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Estimated Time of Arrival: December 31
Solid
10 mg USD 66 In-stock
Estimated Time of Arrival: December 31
50 mg USD 198 In-stock
Estimated Time of Arrival: December 31
100 mg USD 317 In-stock
Estimated Time of Arrival: December 31
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Description

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

Clinical Trial
Molecular Weight

456.32

Formula

C21H23Cl2NO6

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (109.57 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1914 mL 10.9572 mL 21.9144 mL
5 mM 0.4383 mL 2.1914 mL 4.3829 mL
10 mM 0.2191 mL 1.0957 mL 2.1914 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

*All of the co-solvents are available by MCE.
References
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Clevidipine
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