| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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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.
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| ln Vivo |
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| Animal Protocol |
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
urine 63-74%, feces 7-22% Metabolism / Metabolites Clevidipine is rapidly hydrolyzed to inactive metabolites by esterases in arterial blood. Biological Half-Life 1 minute |
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| Toxicity/Toxicokinetics |
Protein Binding
>99.5% |
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| References |
J Pediatr Pharmacol Ther.2015Jan-Feb;20(1):54-60.
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| Additional Infomation |
Clevidipine is a dihydropyridine.
Clevidipine is a dihydropyridine L-type calcium channel blocker that is selective for vascular smooth muscle and is indicated for blood pressure reduction when oral therapy is not an option. Clevidipine is a Dihydropyridine Calcium Channel Blocker. The mechanism of action of clevidipine is as a Calcium Channel Antagonist. Drug Indication For the reduction of blood pressure when when oral antihypertensive therapy is not feasible or not desirable. FDA Label Treatment of hypertensive disease Mechanism of Action Possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, clevidipine inhibits the influx of extracellular calcium across both the myocardial and vascular smooth muscle cell membranes. The resultant inhibition of the contractile processes of the myocardial smooth muscle cells leads to dilation of the coronary and systemic arteries and improved oxygen delivery to the myocardial tissue. Pharmacodynamics Clevidipine belongs to a well-known class of drugs called dihydropyridine calcium channel antagonists. Clevidpine is the first third generation intravenous dihydropyridine calcium channel blocker. In vitro studies demonstrated that clevidipine acts by selectively relaxing the smooth muscle cells that line small arteries, resulting in arterial dilation, widening of the artery opening, and without reducing central venous pressure or reducing cardiac output. |
| 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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