Clevidipine
Based on 1 publication(s) in Google Scholar
Clevidipine is a selective, short-acting L-type calcium channel antagonist with an IC50 of 7.1 nM. Clevidipine can competitively bind to calcium channels and exert rapid vasoselective vasodilation by blocking the influx of extracellular calcium ions, thereby reducing peripheral vascular resistance and effectively controlling acute severe hypertension. Clevidipine can also protect the myocardium from reperfusion injury by promoting the release of nitric oxide (NO). Clevidipine can be used in the research of acute hypertension, perioperative blood pressure management, and myocardial ischemia-reperfusion injury.
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- Purity: 99.59%
- CAS No.: 167221-71-8
- 화학식: C21H23Cl2NO6
- 분자량:456.32
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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용액&용해도
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- References
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Publications Citing Use of MedChemExpress (MCE) Clevidipine
MoreAll Calcium Channel Isoforms
More
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Ventricular myocyte | IC50 |
0.0071 μM
Compound: Celvidipine
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Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
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[PMID: 22761000] |
| Ventricular myocyte | IC50 |
0.0788 μM
Compound: Celvidipine
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Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
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[PMID: 22761000] |
Clevidipine (1.0 mg/kg; intravenous injection; single) shows rapid blood clearance in rats, mainly distributed in the heart and brain, and its metabolite H152/81 has a longer elimination half-life[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pigs with myocardial ischemia-reperfusion model[2]
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Dosage:0.3 nmol/kg/min, 15 min
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Administration:Intracoronary infusion via left anterior descending coronary artery (LAD), single administration for 10 minutes during late ischemia and 5 minutes during early reperfusion
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Result:Significantly reduced infarct size to 59±3% of the area at risk compared to 86±2% in the vehicle group.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 167221-71-8
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Appearance Solid
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분자량 456.32
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화학식 C21H23Cl2NO6
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Color White to off-white
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SMILES
O=C(C1=C(C)NC(C)=C(C(OCOC(CCC)=O)=O)C1C2=CC=CC(Cl)=C2Cl)OC
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Biomed Eng
DeepDrugDiscovery identifies blood-brain barrier permeable autophagy enhancers for Alzheimer's disease. [Abstract]2026 Apr 24. PMID: 42032039
용액&용해도
DMSO : ≥ 50 mg/mL (109.57 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (277 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
[1]. Pollack CV, et al. Clevidipine, an intravenous dihydropyridine calcium channel blocker, is safe and effective for the treatment of patients with acute severe hypertension. Ann Emerg Med. 2009 Mar;53(3):329-38. [Content Brief]
[2]. Gourine A, et al. Short-acting calcium antagonist clevidipine protects against reperfusion injury via local nitric oxide-related mechanisms in the jeopardised myocardium. Cardiovasc Res. 2001 Jul;51(1):100-7. [Content Brief]
[3]. Wang Y, et al. Pharmacokinetics and tissue distribution study of clevidipine and its primary metabolite H152/81 in rats. Biomed Chromatogr. 2018 Feb;32(2). [Content Brief]
[4]. Wiśniowska B, et al. Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment. J Appl Toxicol. 2012 Oct;32(10):858-66. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1914 mL | 10.9572 mL | 21.9144 mL | 54.7861 mL |
| 5 mM | 0.4383 mL | 2.1914 mL | 4.3829 mL | 10.9572 mL | |
| 10 mM | 0.2191 mL | 1.0957 mL | 2.1914 mL | 5.4786 mL | |
| 15 mM | 0.1461 mL | 0.7305 mL | 1.4610 mL | 3.6524 mL | |
| 20 mM | 0.1096 mL | 0.5479 mL | 1.0957 mL | 2.7393 mL | |
| 25 mM | 0.0877 mL | 0.4383 mL | 0.8766 mL | 2.1914 mL | |
| 30 mM | 0.0730 mL | 0.3652 mL | 0.7305 mL | 1.8262 mL | |
| 40 mM | 0.0548 mL | 0.2739 mL | 0.5479 mL | 1.3697 mL | |
| 50 mM | 0.0438 mL | 0.2191 mL | 0.4383 mL | 1.0957 mL | |
| 60 mM | 0.0365 mL | 0.1826 mL | 0.3652 mL | 0.9131 mL | |
| 80 mM | 0.0274 mL | 0.1370 mL | 0.2739 mL | 0.6848 mL | |
| 100 mM | 0.0219 mL | 0.1096 mL | 0.2191 mL | 0.5479 mL |
Clevidipine Related Classifications
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