| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Clevidipine (Cleviprex) is a potent and short acting, dihydropyridine-based L-type calcium channel blocker used for reducing blood pressure when oral therapy is not feasible or not desirable. Clevidipine is highly selective for vascular, as opposed to myocardial, smooth muscle and, therefore, has little or no effect on myocardial contractility or cardiac conduction. It was approved by the FDA on August 1, 2008 as an antihypertensive agent for the reduction of blood pressure.
| Targets |
Calcium channel antagonist [1]
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| ln Vitro |
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
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| ln 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.
In a prospective open-label observational study of 30 pediatric patients (age 7.9-17.4 years) undergoing posterior spinal fusion for neuromuscular scoliosis, Clevidipine was administered to maintain mean arterial pressure (MAP) at 55-65 mmHg when MAP was ≥65 mmHg despite a remifentanil infusion at 0.3 mcg/kg/min. The target MAP was initially achieved at a mean time of 8.9 minutes (median 5 minutes); 53.3% of patients achieved target MAP within 5 minutes. The maintenance infusion rate varied from 0.25 to 5.0 mcg/kg/min (mean 1.4±1.1 mcg/kg/min). The duration of administration varied from 8 to 527 minutes (mean 160±123 minutes). In 6 of 30 patients, the infusion was discontinued due to concerns regarding spinal cord perfusion (3 due to surgeon judgment, 3 due to changes in neurophysiological monitoring which reverted promptly with restoration of BP). Heart rate increased from baseline 83±16 to 86±15 bpm (p=0.04); no patient had HR increase ≥20 bpm or required a β-adrenergic antagonist. In 18 of 30 patients (60%), the infusion was temporarily paused at least once due to MAP <55 mmHg (total 43 pauses, range 1-5 per patient). Only 1 patient required a fluid bolus (4-5 mL/kg) for low MAP; no patient required a vasoactive agent. When the infusion was discontinued, MAP returned to ≥65 mmHg within 10 minutes in 12 of 30 patients (40%). Estimated blood loss was 434±248 mL; 7 of 30 patients (23%) received allogeneic blood transfusion. No significant change in oxygenation (P/F ratio) was noted (539±46 mmHg vs. 541±73 mmHg, p=0.46). [1] |
| Animal Protocol |
PK studies
Rabbit, rat, and dog |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
63-74% in urine, 7-22% in feces. Metabolism/Metabolites Cevidipine is rapidly hydrolyzed into inactive metabolites by esterases in arterial blood. Biological Half-Life 1 minute. Clevidipine has a half-life of 1 to 3 minutes due to rapid metabolism by non-specific blood and tissue esterases. [1] |
| Toxicity/Toxicokinetics |
Protein Binding
99.5% Heart rate increased from baseline 83±16 to 86±15 bpm (p=0.04) with Clevidipine administration; no patient had HR increase ≥20 bpm or required a β-adrenergic antagonist. Excessive hypotension (MAP <55 mmHg) occurred in 18 of 30 patients (60%), requiring temporary pauses of the infusion (total 43 pauses); only 1 patient needed a fluid bolus and no patient required a vasoactive agent. No significant effect on oxygenation (P/F ratio: 539±46 mmHg vs. 541±73 mmHg, p=0.46). Clevidipine is provided in a lipid-based solution; its administration is relatively contraindicated in patients with allergies to soybeans, soy products, eggs, or egg products, or acquired/inherited disorders of lipid metabolism. [1] |
| References |
J Pediatr Pharmacol Ther.2015Jan-Feb;20(1):54-60.
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| Additional Infomation |
Cevidipine is a dihydropyridine drug. Cevidipine is a dihydropyridine L-type calcium channel blocker, selective for vascular smooth muscle, and is indicated for lowering blood pressure when oral antihypertensive drugs are not feasible. Cevidipine is a dihydropyridine calcium channel blocker. The mechanism of action of cevidipine is as a calcium channel antagonist. Drug Indications For lowering blood pressure, especially in cases where oral antihypertensive drugs are not feasible or suitable. FDA Label Treatment of Hypertension Mechanism of Action Cevidipine may inhibit the influx of extracellular calcium ions across the membranes of cardiomyocytes and vascular smooth muscle cells by altering channel structure, inhibiting ion-gated mechanisms, and/or interfering with the release of calcium ions from the sarcoplasmic reticulum. Inhibition of myocardial smooth muscle cell contraction leads to dilation of coronary and systemic arteries, thereby improving oxygen delivery to myocardial tissue. Pharmacodynamics Cevidipine belongs to the well-known class of dihydropyridine calcium channel antagonists. Cevidipine is the first third-generation intravenous dihydropyridine calcium channel blocker. In vitro studies have shown that cevidipine works by selectively relaxing smooth muscle cells in the inner wall of small arteries, thereby causing arterial dilation, widening the arterial opening, without reducing central venous pressure or cardiac output.
Clevidipine is used for controlled hypotension to limit or avoid the need for allogeneic blood transfusion during major orthopedic surgical procedures such as posterior spinal fusion. It preferentially dilates the arterial vasculature, limiting effects on preload and heart rate. Compared to nicardipine, it has a shorter duration of action and easier titratability. The mean time for MAP return to baseline after discontinuation was 7.2±6.7 minutes, which is shorter than reported for nicardipine (18.1±13.5 min, 26.8±4.0 min, median 66.5 min) and similar to nitroprusside (7.3±1.1 min). The reflex tachycardia is dose-related. [1] |
| Molecular Formula |
C21H23CL2NO6
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| Molecular Weight |
456.32
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| Exact Mass |
455.09
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| CAS # |
167221-71-8
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| Related CAS # |
Clevidipine-d7;(R)-Clevidipine-13C,d3
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| PubChem CID |
153994
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
539.7±50.0 °C at 760 mmHg
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| Melting Point |
128-130°C
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| Flash Point |
280.2±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.543
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| LogP |
5.46
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
30
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| Complexity |
748
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KPBZROQVTHLCDU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H23Cl2NO6/c1-5-7-15(25)29-10-30-21(27)17-12(3)24-11(2)16(20(26)28-4)18(17)13-8-6-9-14(22)19(13)23/h6,8-9,18,24H,5,7,10H2,1-4H3
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| Chemical Name |
methyl 5-{[(butanoyloxy)methoxy]carbonyl}-4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3-carboxylate
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.48 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05783557 | Not yet recruiting | Drug: Clevidipine Butyrate Injectable Emulsion Drug: Cleviprex® |
Hypertensive Emergency | CSPC Zhongnuo Pharmaceutical (Shijiazhuang) Co., Ltd. |
May 1, 2023 | Phase 3 |
| NCT00978822 | Terminated | Drug: Clevidipine butyrate injectable emulsion |
Subarachnoid Hemorrhage Hypertension |
Henry Ford Health System | June 2009 | Phase 2 |
| NCT05922436 | Not yet recruiting | Drug: QLG2071 Drug: Cleviprex® |
Hypertensive Emergency | Qilu Pharmaceutical (Hainan) Co., Ltd. |
July 15, 2023 | Phase 3 |
| NCT04670809 | Unknown | Drug: Clevidipine Butyrate Injection Drug: Ncardipine Hydrochloride Injection |
Hypertensive Emergency | Nanjing Yoko Biomedical Co., Ltd. |
July 27, 2020 | Phase 3 |
| NCT01526876 | Withdrawn | Drug: clevidipine butyrate | Hypertension | Columbia University | November 2011 | Phase 4 |
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