Didesmethyl cariprazine
Based on 1 Customer Validation
Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.
For research use only. We do not sell to patients.
- Purity: 99.63%
- CAS No.: 839712-25-3
- Formula: C19H28Cl2N4O
- Molecular Weight:399.36
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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human 5-HT1A Receptor 1.7 nM (Ki) |
Human D3 Receptor 0.056 nM (Ki) |
D2L Receptor 1.41 nM (Ki) |
human 5-HT2B Receptor 0.52 nM (Ki) |
Didesmethyl cariprazine is a partial agonist of D2 and D3 receptors, a full agonist of the 5-HT1A receptor, and an antagonist of the human 5-HT2B receptor (Ki: 1.41 nM (human D2L)), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B))[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 839712-25-3
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Appearance Solid
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Molecular Weight 399.36
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Formula C19H28Cl2N4O
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Color Off-white to light yellow
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SMILES
O=C(N)N[C@H]1CC[C@H](CCN2CCN(C3=CC=CC(Cl)=C3Cl)CC2)CC1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 11.36 mg/mL (28.45 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. 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. 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)
Purity & Documentation
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Data Sheet (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Citrome L, et al. Cariprazine for acute and maintenance treatment of adults with schizophrenia: an evidence-based review and place in therapy. Neuropsychiatr Dis Treat. 2018 Oct 5;14:2563-2577. [Content Brief]
[2]. Kiss B, et al. Preclinical pharmacodynamic and pharmacokinetic characterization of the major metabolites of cariprazine. Drug Des Devel Ther. 2019 Sep 16;13:3229-3248. [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. 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 | 2.5040 mL | 12.5200 mL | 25.0401 mL | 62.6002 mL |
| 5 mM | 0.5008 mL | 2.5040 mL | 5.0080 mL | 12.5200 mL | |
| 10 mM | 0.2504 mL | 1.2520 mL | 2.5040 mL | 6.2600 mL | |
| 15 mM | 0.1669 mL | 0.8347 mL | 1.6693 mL | 4.1733 mL | |
| 20 mM | 0.1252 mL | 0.6260 mL | 1.2520 mL | 3.1300 mL | |
| 25 mM | 0.1002 mL | 0.5008 mL | 1.0016 mL | 2.5040 mL |
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