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Olinone 

Cat. No. M28846
Olinone  Structure
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Biological Activity

Olinone is a selective BRD4 BrD1 inhibitor. Olinone accelerates the progression of mouse primary oligodendrocyte progenitors toward differentiation.

Chemical Information
Molecular Weight 299.37
Formula C17H21N3O2
CAS Number 1770789-37-1
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] J P Hilton-Proctor, et al. Bioorg Med Chem. Synthesis and elaboration of N-methylpyrrolidone as an acetamide fragment substitute in bromodomain inhibition

[2] Yoel Rodríguez, et al. Proteins. In silico design and molecular basis for the selectivity of Olinone toward the first over the second bromodomain of BRD4

[3] Lei Zhao, et al. J Neuroinflammation. Photoreceptor protection via blockade of BET epigenetic readers in a murine model of inherited retinal degeneration

[4] Cheng-Ming Chiang. Chem Biol. Nonequivalent response to bromodomain-targeting BET inhibitors in oligodendrocyte cell fate decision

[5] Mar Gacias, et al. Chem Biol. Selective chemical modulation of gene transcription favors oligodendrocyte lineage progression

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