Desmethyl cariprazine
Based on 1 Customer Validation
Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotonin receptors, showing a pEC50 of 8.90 at human D2 receptors, a pEC50 of 8.09 at D3 receptors, and a pEC50 of 6.28 at 5-HT1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1A receptors, and suppresses serotonin-induced Ca2+ release at 5-HT2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.
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- Pureté: 98.08%
- CAS No.: 839712-15-1
- Formule: C20H30Cl2N4O
- Masse moléculaire:413.38
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Help & FAQs
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Activité biologique
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5-HT1A Receptor |
D3 Receptor 0.085 nM (Ki) |
D2 Receptor 0.49 nM (Ki) |
5-HT1A Receptor 2.6 nM (Ki) |
Desmethyl-cariprazine (1 μM; 10 μM for 70+ other targets) shows a receptor binding profile highly similar to cariprazine, with high affinity for human and rat D3, D2, 5-HT2B, and 5-HT1A receptors, higher D3 vs D2 selectivity than cariprazine, and negligible activity against most other molecular targets[2].
Desmethyl-cariprazine (range of concentrations) acts as a partial agonist at recombinant human D2, D3, and 5-HT1A receptors in cAMP signaling assays, with comparable intrinsic efficacy to cariprazine and didesmethyl-cariprazine at D2 and D3 receptors, but lower intrinsic efficacy and potency than the other two compounds at 5-HT1A receptors[2].
Desmethyl-cariprazine (range of concentrations) acts as a pure antagonist at recombinant human 5-HT2B receptors with high potency, similar to cariprazine and didesmethyl-cariprazine[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 839712-15-1
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Appearance Solid
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Masse moléculaire 413.38
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Formule C20H30Cl2N4O
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Color White to off-white
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SMILES
O=C(NC)N[C@@H]1CC[C@@H](CCN2CCN(C3=CC=CC(Cl)=C3Cl)CC2)CC1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 5 mg/mL (12.10 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)
Pureté et documentation
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Fiche technique (271 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Campbell RH, et al. Review of cariprazine in management of psychiatric illness. Ment Health Clin. 2018 Mar 23;7(5):221-229. [Content Brief]
[2]. Kiss B, et al. Preclinical pharmacodynamic and pharmacokinetic characterization of the major metabolites of cariprazine. Drug Des Devel Ther. 2019;13:3229-3248. Published 2019 Sep 16. [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 | 2.4191 mL | 12.0954 mL | 24.1908 mL | 60.4770 mL |
| 5 mM | 0.4838 mL | 2.4191 mL | 4.8382 mL | 12.0954 mL | |
| 10 mM | 0.2419 mL | 1.2095 mL | 2.4191 mL | 6.0477 mL |
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