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UNC9994 

Cat. No. M28228
UNC9994  Structure
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Biological Activity

UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity.

Chemical Information
Molecular Weight 421.38
Formula C21H22Cl2N2OS
CAS Number 1354030-51-5
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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.

References

[1] Zhoubin Tan, et al. Br J Pharmacol. Exploiting D2 receptor β-arrestin2-biased signalling to suppress tumour growth of pituitary adenomas

[2] Richard Ågren, et al. Int J Neuropsychopharmacol. The Beta-Arrestin-Biased Dopamine D2 Receptor Ligand, UNC9994, Is a Partial Agonist at G-Protein-Mediated Potassium Channel Activation

[3] Thomas F Pack, et al. J Biol Chem. The dopamine D2 receptor can directly recruit and activate GRK2 without G protein activation

[4] Kristoffer Sahlholm, et al. Mol Neurobiol. Antipsychotic-Like Efficacy of Dopamine D2 Receptor-Biased Ligands is Dependent on Adenosine A2A Receptor Expression

[5] John A Allen, et al. Proc Natl Acad Sci U S A. Discovery of β-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy

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Keywords: UNC9994  supplier, Dopamine Receptor, inhibitors, activators


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