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Odanacatib (MK-0822)

In stock
Catalog No.
A2487
Cathepsin K,potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$170.00
In stock
5mg
$100.00
In stock
10mg
$160.00
In stock
50mg
$400.00
In stock
100mg
$1,000.00
In stock

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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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt525.56
Cas No.603139-19-1
FormulaC25H27F4N3O3S
Solubility≥17.7mg/mL in DMSO
Chemical Name(2S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide
SDFDownload SDF
Canonical SMILESCC(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
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

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          

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