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MLS1082 

Cat. No. M30806
MLS1082  Structure
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Biological Activity

MLS1082 is a pyrimidone-based D1-like dopamine receptor positive allosteric modulator, with an EC50 of 123 nM for DA-stimulated G protein signaling.

Chemical Information
Molecular Weight 385.46
Formula C24H23N3O2
CAS Number 883958-36-9
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] Kathryn D Luderman, et al. Bioorg Med Chem Lett. Development of pyrimidone D1 dopamine receptor positive allosteric modulators

[2] Kathryn D Luderman, et al. Mol Pharmacol. Identification of Positive Allosteric Modulators of the D1 Dopamine Receptor That Act at Diverse Binding Sites

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  Catalog
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Keywords: MLS1082  supplier, Dopamine Receptor, inhibitors, activators


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