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G-744 

Cat. No. M28212
G-744  Structure
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Quality Control & Documentation
Biological Activity

G-744 is a highly potent, selective and orally active Btk inhibitor with an IC50 of 2 nM. G-744 is metabolically stable, well tolerated and efficacious to treat arthritis.

Chemical Information
Molecular Weight 527.64
Formula C29H29N5O3S
CAS Number 1346669-54-2
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] Xiaojing Wang, et al. ACS Med Chem Lett. Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties

[2] Arna Katewa, et al. JCI Insight. Btk-specific inhibition blocks pathogenic plasma cell signatures and myeloid cell-associated damage in IFN α-driven lupus nephritis

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  Catalog
Abmole Inhibitor Catalog




Keywords: G-744  supplier, BTK, inhibitors, activators


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