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Didesmethyl cariprazine

CAT: 0804-HY-100658-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-100658-01Size:5 mg
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Description
Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine. 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[1][2].
CAS Number
839712-25-3
UNSPSC
12352005
Target
5-HT Receptor; Dopamine Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein; Neuronal Signaling
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/didesmethyl-cariprazine.html
Concentration
10mM
Purity
99.63
Solubility
DMSO : 11.36 mg/mL (ultrasonic; warming; heat to 80°C)
Smiles
O=C(N)N[C@H]1CC[C@H](CCN2CCN(C3=CC=CC(Cl)=C3Cl)CC2)CC1
Molecular Formula
C19H28Cl2N4O
Molecular Weight
399.36
References & Citations
[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.|[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
5-HT1 Receptor;5-HT2 Receptor; D2 Receptor; D3 Receptor