Odanacatib (MK-0822)

Catalog No.S1115

Odanacatib (MK-0822) Chemical Structure

Molecular Weight(MW): 525.56

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. Phase 3.

Size Price Stock Quantity  
In DMSO USD 570 In stock
USD 270 In stock
USD 470 In stock
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Choose Selective Cysteine Protease Inhibitors

Biological Activity

Description 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. Phase 3.
Features A potent, selective, and neutral cathepsin K inhibitor.
Targets
Cathepsin K (human) [1] Cathepsin K (rabbit) [1]
0.2 nM 1 nM
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. [1] A recent study shows that Odanacatib results in reduction of Osteoclast (OC) resorption activity by interrupting intracellular vesicular trafficking. [2]

In vivo In 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. [1] 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%). [3] In the estrogen-deficient, skeletally mature rhesus monkeys, long-term treatment with Odanacatib effectively inhibits bone turnover without reducing osteoclast number and maintains normal biomechanical properties of the spine of OVX nonhuman primates. [4]

Protocol

Animal Research:[3]
+ Expand
  • Animal Models: Ovariectomized (OVX) rabbit model
  • Formulation: Odanacatib is provided in a diet formulae.
  • Dosages: ≤9 µM/day
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (190.27 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
4% DMSO+corn oil
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 525.56
Formula

C25H27F4N3O3S

CAS No. 603139-19-1
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01803607 Terminated Osteoporosis Merck Sharp & Dohme Corp. March 2013 Phase 3
NCT01630616 Terminated Osteoporosis Merck Sharp & Dohme Corp. March 2013 Phase 1
NCT01552122 Withdrawn Osteoporosis|Postmenopausal Osteoporosis Merck Sharp & Dohme Corp. May 2012 Phase 3
NCT01512693 Completed Hepatic Insufficiency Merck Sharp & Dohme Corp. February 2012 Phase 1
NCT01512667 Completed Renal Insufficiency Merck Sharp & Dohme Corp. January 2012 Phase 1
NCT01120600 Completed Osteoporosis Merck Sharp & Dohme Corp. June 2010 Phase 3

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID