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Odanacatib (MK-0822)Cathepsin K,potent and selective

Odanacatib (MK-0822)

Catalog No. A2487
Size Price Stock Qty
5mg $100.00 In stock
50mg $400.00 In stock
100mg $1,000.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Odanacatib (MK-0822)

Biological Activity

A potent and selective inhibitor of cysteine protease cathepsin K (IC50 0.2 nM), discriminating against cathepsin B (1034 nM), L (2995 nM), and S (60 nM)
Targets cathepsin K          
IC50 0.2nM          

Odanacatib (MK-0822) Dilution Calculator

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Chemical Properties

Cas No. 603139-19-1 SDF Download SDF
Chemical Name (2S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide
Canonical SMILES CC(C)(CC(C(=O)NC1(CC1)C#N)NC(C2=CC=C(C=C2)C3=CC=C(C=C3)S(=O)(=O)C)C(F)(F)F)F
Formula C25H27F4N3O3S M.Wt 525.56
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Odanacatib (MK-0822) is a potent, orally active and selective inhibitor of Cathepsin K with IC50 value of 0.20 nM [1],

Cathepsin K is expressed predominantly in osteoclasts and degrades the collagen matrix componentsofbone. It plays a central role in mediating bone resorption. And the inhibitor of cathepsin K, Odanacatib, is in development for the treatment of osteoporosis. Based on preclinical evidence and available clinical data from dose-ranging phase IIB trials, odanacatib appears to reduce bone resorptionwhile somewhat preserving bone formation in postmenopausal

Women. Currently, Odanacatib is undergoing evaluation for fracture risk reduction in a phase III trial with >16000 patients with postmenopausal osteoporosis [2].

References:
[1] S. Aubrey Stoch, Stefan Zajic, Julie A. Stone, Deborah L. Miller, Lucas van Bortel, Kenneth C. Lasseter, Barnali Pramanik, Caroline Cilissen, Qi Liu, Lida Liu, Boyd B. Scott, Deborah Panebianco, Yu Ding, Keith Gottesdiener & John A. Wagner. Odanacatib, a selective cathepsin K inhibitor to treat osteoporosis: safety, tolerability, pharmacokinetics and pharmacodynamics –results from single oral dose studies in healthy volunteers. British Journal of Clinical Pharmacology. 2012, 75, (5): 1240-1254.
[2] Matt S. Anderson, Isaias Noel Gendrano, Chengcheng Liu, Steven Jeffers,

Chantal Mahon, Anish Mehta, Kate Mostoller, Stefan Zajic, Denise Morris, Jessie Lee, and S. Aubrey Stoch. Odanacatib, a selective Cathepsin K inhibitor, demonstrates comparable pharmacodynamics and pharmacokinetics in older men and postmenopausal women. Endocrine Research. 2014, 99(2):552–560.