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MK-8189 

Cat. No. M28395
MK-8189  Structure
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Biological Activity

MK-8189 is a potent, orally active and selective PDE10A inhibitor with a Ki value of 29 pM. MK-8189 can be used in research of schizophrenia.

Chemical Information
Molecular Weight 382.48
Formula C19H22N6OS
CAS Number 1424371-93-6
Form Solid
Solubility (25°C) DMSO 125 mg/mL (ultrasonic)
Storage Powder -20°C
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] Michal R Tomaszewski, et al. J Lipid Res. Magnetic resonance imaging detects white adipose tissue beiging in mice following PDE10A inhibitor treatment

[2] Mark E Layton, et al. J Med Chem. Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia

[3] Maria C Lobo, et al. Neurosci Biobehav Rev. New and emerging treatments for schizophrenia: a narrative review of their pharmacology, efficacy and side effect profile relative to established antipsychotics

[4] Amanda Krogmann, et al. CNS Spectr. Keeping up with the therapeutic advances in schizophrenia: a review of novel and emerging pharmacological entities

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  Catalog
Abmole Inhibitor Catalog




Keywords: MK-8189  supplier, PDE, inhibitors, activators


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