| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg | |||
| Other Sizes |
| Targets |
Clebopride malate is a dopamine D2 receptor antagonist. It selectively binds to D2 dopamine receptors with a Ki of 3.5 nM in bovine brain membranes. By blocking D2 receptors in the gastrointestinal tract and smooth muscle, it enhances gastrointestinal motility and alleviates dyspepsia symptoms. The compound also binds to α2 adrenergic receptors with a Ki of 780 nM. Its antiemetic and prokinetic effects are mediated through D2 receptor antagonism.
|
|---|---|
| ln Vitro |
In vitro, Clebopride malate (0.1 nM-10 μM, 30 min) selectively binds to D2 dopamine receptors (Ki: 3.5 nM) and α2 adrenergic receptors (Ki: 780 nM) in bovine brain membranes. It inhibits ETS-induced gastric strip contractions with an IC50 of 0.43 μM. The compound demonstrates antiemetic and prokinetic effects in cell-based and tissue-based assays. Its binding affinity and functional activity have been characterized in various in vitro systems.
|
| ln Vivo |
In vivo, Clebopride malate is orally active and has been used in the study of functional gastrointestinal disorders. As a dopamine D2 receptor antagonist, it enhances gastrointestinal motility and alleviates dyspepsia symptoms. The compound has antiemetic and prokinetic effects. It is used to treat functional gastrointestinal disorders such as nausea or vomiting. Further in vivo studies have evaluated its efficacy in gastrointestinal motility disorders.
|
| Enzyme Assay |
In vitro receptor binding assays for Clebopride malate involve measuring affinity for D2 dopamine receptors and α2 adrenergic receptors. Radioligand binding displacement studies are performed using membranes from bovine brain or cells expressing recombinant receptors. The compound's Ki values (3.5 nM for D2, 780 nM for α2) are determined through competitive binding assays. Functional antagonism is assessed by measuring inhibition of dopamine-induced signaling or tissue contractions. For gastric strip contraction assays, tissue strips are mounted in organ baths and contractions are induced by electrical stimulation (ETS). Assays are performed in appropriate buffer systems with positive controls such as known D2 antagonists (e.g., haloperidol).
|
| Cell Assay |
Clebopride malate cell-based assays are conducted in cells expressing dopamine D2 receptors. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with the compound at varying concentrations (0.1 nM-10 μM). Receptor binding is assessed by radioligand displacement. Functional activity is assessed by measuring inhibition of cAMP accumulation or calcium mobilization. Cell viability is assessed by standard assays. Tissue-based assays using gastric strips are performed to assess inhibition of contractions (IC50: 0.43 μM). Experiments are performed in triplicate with appropriate positive and negative controls.
|
| Animal Protocol |
Clebopride malate in vivo studies are conducted in animal models of gastrointestinal disorders. Animals are treated with Clebopride malate via oral administration. Gastrointestinal motility is assessed by measuring gastric emptying, intestinal transit, or colonic motility. For antiemetic studies, animal models of emesis (e.g., cisplatin-induced emesis in ferrets or shrews) are used. Dosing regimens are optimized based on pharmacokinetic data. Animals are monitored for clinical signs. Tissues and blood samples are collected for histopathological and biomarker analysis at study endpoints. Studies are conducted in accordance with institutional animal care guidelines.
|
| ADME/Pharmacokinetics |
Clebopride malate (MW 507.96 g/mol, C24H30ClN3O7) is an orally active dopamine receptor antagonist. It is soluble in water (8.33 mg/mL with ultrasonic) and DMSO (60 mg/mL with ultrasonic). The compound has a purity of >98%. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in species-specific studies. The compound is used in research on functional gastrointestinal disorders.
|
| Toxicity/Toxicokinetics |
Clebopride malate is generally well-tolerated in preclinical studies at therapeutic doses. The compound is a dopamine receptor antagonist with established safety profiles. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
|
| Additional Infomation |
Clebopride malate is an orally active dopamine receptor antagonist that acts on dopamine D2 receptors with antiemetic and prokinetic effects. It selectively binds to D2 receptors with a Ki of 3.5 nM. The compound inhibits ETS-induced gastric strip contractions with an IC50 of 0.43 μM. Clebopride malate is used in the study of functional gastrointestinal disorders. Its molecular formula is C24H30ClN3O7 with a molecular weight of 507.96 g/mol. All applications are limited to non-human research use.
|
| Molecular Formula |
C20H25N3O2CL+.C4H5O5-
|
|---|---|
| Molecular Weight |
507.9639
|
| Exact Mass |
507.177
|
| CAS # |
57645-91-7
|
| PubChem CID |
14178874
|
| Appearance |
Typically exists as solid at room temperature
|
| Boiling Point |
514.7ºC at 760 mmHg
|
| Flash Point |
265.1ºC
|
| LogP |
2.021
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
35
|
| Complexity |
579
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(O)C(O)CC(O)=O.O=C(NC1CCN(CC2=CC=CC=C2)CC1)C3=CC(Cl)=C(N)C=C3OC
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~60 mg/mL (~118.12 mM)
H2O : ~8.33 mg/mL (~16.40 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (5.91 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 30.0 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: ≥ 3 mg/mL (5.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3 mg/mL (5.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9687 mL | 9.8433 mL | 19.6866 mL | |
| 5 mM | 0.3937 mL | 1.9687 mL | 3.9373 mL | |
| 10 mM | 0.1969 mL | 0.9843 mL | 1.9687 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
