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TASP0376377 

Cat. No. M27999
TASP0376377  Structure
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Biological Activity

TASP0376377 is a potent and selective CRTH2 antagonist (IC50: 13 nM). TASP0376377 has binding affinity for CRTH2 (IC50: 19 nM).

Chemical Information
Molecular Weight 479.31
Formula C25H16Cl2N2O4
CAS Number 1233246-60-0
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] Rie Nishikawa-Shimono, et al. Bioorg Med Chem. Isoquinoline derivatives as potent CRTH2 antagonists: design, synthesis and SAR

[2] Rie Nishikawa-Shimono, et al. Bioorg Med Chem Lett. Isoquinoline derivatives as potent CRTH2 receptor antagonists: synthesis and SAR

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  Catalog
Abmole Inhibitor Catalog




Keywords: TASP0376377  supplier, Prostaglandin Receptor, inhibitors, activators


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