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PF-06412562

Cat. No. M8114
PF-06412562 Structure
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Biological Activity

PF-06412562 is a dopamine receptor D1 (DRD1) agonist ligand.

Chemical Information
Molecular Weight 331.37
Formula C19H17N5O
CAS Number 1609258-91-4
Solubility (25°C) DMSO: 30 mg/mL
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.

References

[1] Xuemei Huang, et al. The D1/D5 Dopamine Partial Agonist PF-06412562 in Advanced-Stage Parkinson's Disease: A Feasibility Study

[2] Rita Balice-Gordon, et al. A Neurofunctional Domains Approach to Evaluate D1/D5 Dopamine Receptor Partial Agonism on Cognition and Motivation in Healthy Volunteers With Low Working Memory Capacity

[3] Alexander Soutschek, et al. Dopaminergic D 1 Receptor Stimulation Affects Effort and Risk Preferences

[4] Estibaliz Arce, et al. A novel approach to evaluate the pharmacodynamics of a selective dopamine D1/D5 receptor partial agonist (PF-06412562) in patients with stable schizophrenia

[5] Spyros Papapetropoulos, et al. Evaluation of D1/D5 Partial Agonist PF-06412562 in Parkinson's Disease following Oral Administration

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