1308278-50-3
Chemical Structure
Cariprazine-d8
Synonym(s): RGH-188 d8
- CAS No.: 1308278-50-3
- Formula:C21H24D8Cl2N4O
- Molecular Weight:435.46
IUPAC Name: 3-((1r,4r)-4-(2-(4-(2,3-dichlorophenyl)piperazin-1-yl-2,2,3,3,5,5,6,6-d8)ethyl)cyclohexyl)-1,1-dimethylurea
InChIKey: KPWSJANDNDDRMB-OMZDLYIGSA-N
SMILES: ClC1=C(C=CC=C1Cl)N2C([2H])([2H])C([2H])([2H])N(C([2H])([2H])C2([2H])[2H])CC[C@@H]3CC[C@H](CC3)NC(N(C)C)=O
Biological Activity: Cariprazine-d8 is a deuterium labeled Cariprazine. Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Cariprazine-d8 | 98.77% | Cariprazine-d8 is a deuterium labeled Cariprazine. Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM). | ||||||||||||||||||||
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Cariprazine (Standard) | ≥98% | Cariprazine (Standard) is the analytical standard of Cariprazine. This product is intended for research and analytical applications. Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM). | ||||||||||||||||||||
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Cariprazine-d6 | 98.74% | Cariprazine-d6 is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM). | ||||||||||||||||||||
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Cariprazine-d8 | Cariprazine-d8-1 (RGH-188-d8-1) is the deuterium labeled Cariprazine (HY-14763). Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM). | |||||||||||||||||||||
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Cariprazine | 99.67% | Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM). | ||||||||||||||||||||
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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-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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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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Didesmethyl cariprazine | 99.63% | 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. | ||||||||||||||||||||
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Didesmethyl cariprazine-d8 | 99.40% | Didesmethyl cariprazine-d8 is the deuterium labeled Didesmethyl cariprazine (HY-100658). 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. | ||||||||||||||||||||
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Aripiprazole-d8 | 98.35% | Aripiprazole-d8 (OPC-14597-d8) is the deuterium labeled Aripiprazole (HY-14546). Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19. | ||||||||||||||||||||
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Cariprazine hydrochloride | 99.88% | Cariprazine hydrochloride is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM). | ||||||||||||||||||||
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Dopamine D3 receptor ligand-5 | Dopamine D3 receptor ligand-5 (13a), a Cariprazine (HY-14763) analogue, is a dopamine D3 receptor ligand, with Ki values of 2.85 nM and 0.14 nM for D2R and D3R, respectively. | |||||||||||||||||||||
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Raxlaprazine etomoxil | Raxlaprazine etomoxil is a small molecule compound with dopamine D2 and D3 receptor modulating activity, which has potential application value in research related to mental illnesses. Raxlaprazine etomoxil exhibits high affinity for human recombinant D2L receptors, with an inhibition constant (Ki) of 1.95 nM. Raxlaprazine etomoxil effectively inhibits forskolin-stimulated cAMP accumulation, with an half maximal effective concentration (EC50) of 3.72 nM in functional activity experiments. | |||||||||||||||||||||
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Dopamine D3 receptor agonist-2 | Dopamine D3 receptor agonist-2 is a selective dopamine D3 receptor partial agonist with a Ki of 0.268 nM. Dopamine D3 receptor agonist-2 exhibits 29-fold selectivity over dopamine D2 receptor (Ki= 7.67nM). | |||||||||||||||||||||
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Cariprazine impurity 1 | Cariprazine impurity 1 is a dopamine D2 receptor (D2R) agonist. Cariprazine impurity 1 modulates D2R-mediated Gi/o signaling pathway to inhibit cAMP production, and regulates D2R-mediated β-arrestin2 recruitment pathway. | |||||||||||||||||||||
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Cariprazine N-oxide | Cariprazine N-oxide (Compound DP-3) is the mono-oxidative degradation product of Cariprazine hydrochloride (HY-14763A). Cariprazine hydrochloride exhibits antipsychotic activity. | |||||||||||||||||||||
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