839712-15-1
Chemical Structure
Desmethyl cariprazine
- CAS No.: 839712-15-1
- Formula:C20H30Cl2N4O
- Molecular Weight:413.38
IUPAC Name: 1-((1r,4r)-4-(2-(4-(2,3-dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-3-methylurea
InChIKey: WMQLLTKSISGWHQ-WKILWMFISA-N
SMILES: O=C(NC)N[C@@H]1CC[C@@H](CCN2CCN(C3=CC=CC(Cl)=C3Cl)CC2)CC1
Biological Activity: 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.[1][2]
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Desmethyl cariprazine | 98.08% | 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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Desmethyl cariprazine (Standard) | ≥98% | Desmethyl cariprazine (Standard) is the analytical standard of Desmethyl cariprazine (HY-100656). This product is intended for research and analytical applications. Desmethyl cariprazine is an active metabolite of Cariprazine. Cariprazine, an antipsychotic agent candidate, exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM). | ||||||||||||||||||||
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Desmethyl cariprazine-d8 | 99.90% | Desmethyl cariprazine-d8 is the deuterium labeled Desmethyl cariprazine (HY-100656). 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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References
- [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]
