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Cariprazine

Cat. No. M9601
Cariprazine Structure
Synonym:

RGH-188; MP-214

Size Price Availability
10mg USD 217.8  USD242 4-7 Days
25mg USD 412.2  USD458 4-7 Days
50mg USD 687.6  USD764 4-7 Days
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Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 427.41
Formula C21H32Cl2N4O
CAS Number 839712-12-8
Purity >98.5%
Solubility DMSO 10 mM
Storage at -20°C
References

Cariprazine Exerts Antimanic Properties and Interferes With Dopamine D2 Receptor β-arrestin Interactions
Yonglin Gao, et al. Pharmacol Res Perspect. 2015 Feb;3(1):e00073. PMID: 25692006.

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
Nicholas Seneca, et al. Psychopharmacology (Berl). 2011 Dec;218(3):579-87. PMID: 21625907.

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
Bela Kiss, et al. J Pharmacol Exp Ther. 2010 Apr;333(1):328-40. PMID: 20093397.

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

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