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(MK-0822; MK 0822; MK0822)
Odanacatib Chemical Structure
|Product name: Odanacatib|
|Cat. No.: HY-10042|
Odanacatib (MK 0822) is a potent, selective, and neutral inhibitor of cathepsin K (human/rabbit) with IC50 of 0.2 nM/1 nM, and demonstrated high selectivity versus off-target cathepsin B, L, S.
IC50 value: 0.2 nM/1 nM(human/rabbi cathepsin K)
in vitro: In vitro, Odanacatib shows the high inhibitory activity and selectivity on cathepsin K with IC50 values of 0.2 nM and 1 nM for human cathepsin K and rabbit cathepsin K, respectively. Furthermore, Odanacatib also shows similar potencies in whole human cell enzyme occupancy assays with corrected IC50 of 5 nM. A recent study shows that Odanacatib results in reduction of Osteoclast (OC) resorption activity by interrupting intracellular vesicular trafficking.
in vivo: n preclinical rats, Odanacatib (10 mg/kg) exhibits excellent pharmacokinetics with clearance (Cl: 2 mL kg-1 min-1), low volume of distribution (Vdss: 1.1 L kg-1), half-life (T1/2: 6 hours) and oral bioavailability (F: 8%), respectively. Besides, Odanacatib also exhibits excellent metabolic stability in rat hepatocytes with a 96% recovery of the parent identity. Odanacatib (ODN) administrated by p.o. prevents bone loss in ovariectomized (OVX) rabbits in a dose-related manner. Moreover, Odanacatib (9?μM/day) leads to a significant increase in proximal femur bone mineral density (BMD) (7.8%), femoral neck BMD (10.8%) and the greater trochanter BMD (6.5%).
|M.Wt||525.56||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||1.9027 mL||9.5137 mL||19.0273 mL|
|5 mM||0.3805 mL||1.9027 mL||3.8055 mL|
|10 mM||0.1903 mL||0.9514 mL||1.9027 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|Odanacatib||Merck & Co Inc||Postmenopausal osteoporosis||31-MAR-13||30-SEP-15||Phase 3||18-MAY-13|
|Merck & Co Inc||Osteoporosis||31-JUL-10||31-JUL-13||Phase 3||15-NOV-13|
|Merck & Co Inc||Hormone refractory prostate cancer||04-JUN-08||31-AUG-08||Phase 3||15-JUN-10|
|Merck & Co Inc||Osteoporosis||31-MAY-12||28-FEB-15||Phase 3||11-SEP-13|
|Merck & Co Inc||Breast tumor||04-JUN-08||31-AUG-08||Phase 3||19-DEC-08|
. Jacques Yves Gauthier, Nathalie ChauretThe discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K Bioorganic & Medicinal Chemistry Letters Volume 18, Issue 3, 1 February 2008, Pages 923-928
Odanacatib is a potent, selective, and neutral cathepsin K inhibitor which was developed to address the metabolic liabilities of the Cat K inhibitor L-873724. Substituting P1 and modifying the P2 side chain led to a metabolically robust inhibitor with a long half-life in preclinical species. Odanacatib was more selective in whole cell assays than the published Cat K inhibitors balicatib and relacatib. Evaluation in dermal fibroblast culture showed minimal intracellular collagen accumulation relative to less selective Cat K inhibitors....
. Langdahl B, Binkley N, Bone H, Gilchrist N, Resch H, Portales JR, Denker A, Lombardi A, De Tilleghem CL, Dasilva C, Rosenberg E, Leung A.Odanacatib in the treatment of postmenopausal women with low bone mineral density: 5 years of continued therapy in a phase 2 study.J Bone Miner Res. 2012 Jul 6.
. Sun L, Forni S, Schwartz MS, Breidinger S, Woolf EJ.Quantitative determination of odanacatib in human plasma using liquid-liquid extraction followed by liquid chromatography-tandem mass spectrometry analysis.J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Feb 15;885-886:15-23. Epub 2011 Dec 13.
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