Clebopride malate
Based on 1 publication(s) in Google Scholar
Clebopride malate is an orally active dopamine Receptor antagonist. Clebopride malate acts on dopamine D2 receptors and has antiemetic and prokinetic effects. Clebopride malate can be used in the study of functional gastrointestinal disorders.
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- Pureté: 99.41%
- CAS No.: 57645-91-7
- Formule: C24H30ClN3O7
- Masse moléculaire:507.96
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Clebopride malate
MoreVoir tous les produits spécifiques à Isoform Dopamine Receptor
MoreVoir tous les produits spécifiques à Isoform Adrenergic Receptor
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Activité biologique
Clebopride malate (0.1 nM-10μM, 30 min) selectively binds to D2 dopamine receptors (Ki: 3.5 nM) and α2 adrenergic receptors (Ki: 780 nM) in bovine brain membranes[3].
Clebopride malate inhibits ETS-induced gastric strip contractions (IC50: 0.43 μM) [3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 57645-91-7
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Appearance Solid
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Masse moléculaire 507.96
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Formule C24H30ClN3O7
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Color White to off-white
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SMILES
O=C(O)C(O)CC(O)=O.O=C(NC1CCN(CC2=CC=CC=C2)CC1)C3=CC(Cl)=C(N)C=C3OC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Metab
Imatinib and methazolamide ameliorate COVID-19-induced metabolic complications via elevating ACE2 enzymatic activity and inhibiting viral entry. [Abstract]2022 Mar 1;34(3):424-440.e7. PMID: 35150639
Solvant et solubilité
DMSO : 60 mg/mL (118.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 8.33 mg/mL (16.40 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 3 mg/mL (5.91 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (5.91 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (sealed storage, away from moisture)
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.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Reis-Carneiro D, et al. Clebopride-Associated Movement Disorders. Mov Disord Clin Pract. 2023 Sep 6;10(10):1562-1563. [Content Brief]
[2]. Elliott PN, et al. Substituted benzamides as cerebral dopamine antagonists in rodents. Neuropharmacology. 1977 May;16(5):333-42. [Content Brief]
[3]. Takeda K, et al. Clebopride enhances contractility of the guinea pig stomach by blocking peripheral D2 dopamine receptor and alpha-2 adrenoceptor. J Pharmacol Exp Ther. 1991 May;257(2):806-11. [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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.9687 mL | 9.8433 mL | 19.6866 mL | 49.2165 mL |
| 5 mM | 0.3937 mL | 1.9687 mL | 3.9373 mL | 9.8433 mL | |
| 10 mM | 0.1969 mL | 0.9843 mL | 1.9687 mL | 4.9216 mL | |
| 15 mM | 0.1312 mL | 0.6562 mL | 1.3124 mL | 3.2811 mL | |
| DMSO | 20 mM | 0.0984 mL | 0.4922 mL | 0.9843 mL | 2.4608 mL |
| 25 mM | 0.0787 mL | 0.3937 mL | 0.7875 mL | 1.9687 mL | |
| 30 mM | 0.0656 mL | 0.3281 mL | 0.6562 mL | 1.6405 mL | |
| 40 mM | 0.0492 mL | 0.2461 mL | 0.4922 mL | 1.2304 mL | |
| 50 mM | 0.0394 mL | 0.1969 mL | 0.3937 mL | 0.9843 mL | |
| 60 mM | 0.0328 mL | 0.1641 mL | 0.3281 mL | 0.8203 mL | |
| 80 mM | 0.0246 mL | 0.1230 mL | 0.2461 mL | 0.6152 mL | |
| 100 mM | 0.0197 mL | 0.0984 mL | 0.1969 mL | 0.4922 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Clebopride malate Related Classifications
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