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GW-3333 

Cat. No. M29272
GW-3333  Structure
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Biological Activity

GW-3333 is a potent and orally active TNF-alpha-converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitor. GW-3333 inhibits tumor necrosis factor-alpha (TNF-alpha) production and arthritis.

Chemical Information
Molecular Weight 420.55
Formula C22H36N4O4
CAS Number 212609-68-2
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] Andrea E Tóth, et al. Arch Med Res. Compounds blocking methylglyoxal-induced protein modification and brain endothelial injury

[2] Timothy K Tippin, et al. Drug Metab Dispos. CYP3A induction by N-hydroxyformamide tumor necrosis factor-alpha converting enzyme/matrix metalloproteinase inhibitors use of a pregname X receptor activation assay and primary hepatocyte culture for assessing induction potential in humans

[3] Sheila A Doggrell. Expert Opin Investig Drugs. TACE inhibition: a new approach to treating inflammation

[4] M H Rabinowitz, et al. J Med Chem. Design of selective and soluble inhibitors of tumor necrosis factor-alpha converting enzyme (TACE)

[5] J G Conway, et al. J Pharmacol Exp Ther. Inhibition of tumor necrosis factor-alpha (TNF-alpha) production and arthritis in the rat by GW3333, a dual inhibitor of TNF-alpha-converting enzyme and matrix metalloproteinases

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Keywords: GW-3333  supplier, TNF Receptor, inhibitors, activators


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