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GDC-2394

Cat. No. M21531
GDC-2394  Structure
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Biological Activity

GDC-2394 is an oral inhibitor of NLRP3 inflammasome. The NLRP3 inflamome, the best studied and most characterized, also inhibits IL-1β with IC50 of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β).

Chemical Information
Molecular Weight 431.51
Formula C20H25N5O4S
CAS Number 2238822-07-4
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Christopher McBride, et al. J Med Chem. Overcoming Preclinical Safety Obstacles to Discover ( S)- N-((1,2,3,5,6,7-Hexahydro- s-indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5 H-pyrazolo[5,1- b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor

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Keywords: GDC-2394 supplier, NLR, inhibitors, activators


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