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Cat. No. M9601
Cariprazine Structure

RGH-188; MP-214

Size Price Availability
10mg USD 242  USD242 4-7 Days
25mg USD 458  USD458 4-7 Days
50mg USD 764  USD764 4-7 Days
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Quality Control & Documentation
Biological Activity

Cariprazine is a D2 and D3 receptor partial agonist, with high selectivity towards the D3 receptor. Cariprazine 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). Cariprazine has lower affinity at human and rat hippocampal 5-HT1A receptors (pKi 8.59 and 8.34, respectively) and demonstrates low intrinsic efficacy. Administration of Cariprazine (30 µg/kg) reduces the striatal uptake of both radioligands to the level of nonspecific binding compared with baseline PET measurements.

Chemical Information
Molecular Weight 427.41
Formula C21H32Cl2N4O
CAS Number 839712-12-8
Solubility (25°C) DMSO 10 mM
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Yonglin Gao, et al. Pharmacol Res Perspect. Cariprazine Exerts Antimanic Properties and Interferes With Dopamine D2 Receptor β-arrestin Interactions

[2] Nicholas Seneca, et al. Psychopharmacology (Berl). Occupancy of Dopamine D₂ and D₃ and Serotonin 5-HT₁A Receptors by the Novel Antipsychotic Drug Candidate, Cariprazine (RGH-188), in Monkey Brain Measured Using Positron Emission Tomography

[3] Bela Kiss, et al. J Pharmacol Exp Ther. Cariprazine (RGH-188), a Dopamine D(3) Receptor-Preferring, D(3)/D(2) Dopamine Receptor Antagonist-Partial Agonist Antipsychotic Candidate: In Vitro and Neurochemical Profile

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Keywords: Cariprazine, RGH-188; MP-214 supplier, Dopamine Receptor, inhibitors, activators

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