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L-873724 

Cat. No. M30349
L-873724  Structure
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Biological Activity

L-873724 is a potent, orally bioavailable, selective and reversible[2] non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively. L-873724 also exhibits an IC50 of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption.

Chemical Information
Molecular Weight 481.53
Formula C23H26F3N3O3S
CAS Number 603139-12-4
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage 4°C, protect from light, dry, sealed
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] Brenda L Pennypacker, et al. BMC Musculoskelet Disord. Cathepsin K inhibitors increase distal femoral bone mineral density in rapidly growing rabbits

[2] Sylvie Desmarais, et al. Biol Chem. Pharmacological inhibitors to identify roles of cathepsin K in cell-based studies: a comparison of available tools

[3] Jacques Yves Gauthier, et al. Bioorg Med Chem Lett. The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K

[4] Sylvie Desmarais, et al. Mol Pharmacol. Effect of cathepsin k inhibitor basicity on in vivo off-target activities

[5] W Cameron Black, et al. Chembiochem. The consequences of lysosomotropism on the design of selective cathepsin K inhibitors

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Abmole Inhibitor Catalog




Keywords: L-873724  supplier, Cathepsin, inhibitors, activators

 
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