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    Odanacatib (MK0822)
    Odanacatib (MK0822)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0696
    CAS #: 603139-19-1Purity ≥98%

    Description: Odanacatib (also known as MK-0822) is a potent, selective, and neutral inhibitor of cathepsin K (human/rabbit) with the potential to be used for the treatment for osteoporosis and bone metastasis. It inhibits cathepsin K (human/rabbit) with IC50s of 0.2 nM/1 nM, and exhibited high selectivity over off-target cathepsin B, L, S. Odanacatib selectively binds to and inhibits the activity of cathepsin K, which may result in a reduction in bone resorption, improvement of bone mineral density, and a reversal in osteoporotic changes. Currently, Odanacatib is undergoing evaluation for fracture risk reduction in a phase III trial with >16000 patients with postmenopausal osteoporosis.

    References: Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8; J Bone Miner Res. 2011 Feb;26(2):252-62

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    Molecular Weight (MW)525.56
    FormulaC25H27F4N3O3S
    CAS No.603139-19-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (190.3 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)4% DMSO+corn oil: 5 mg/mL
    SynonymsMK 0822; Odanacatib; MK0822; MK-0822;  

    Chemical Name: (S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-(((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)ethyl)amino)pentanamide

    InChi Key: FWIVDMJALNEADT-SFTDATJTSA-N

    InChi Code: InChI=1S/C25H27F4N3O3S/c1-23(2,26)14-20(22(33)32-24(15-30)12-13-24)31-21(25(27,28)29)18-6-4-16(5-7-18)17-8-10-19(11-9-17)36(3,34)35/h4-11,20-21,31H,12-14H2,1-3H3,(H,32,33)/t20-,21-/m0/s1

    SMILES Code: CC(C)(F)C[[email protected]](N[[email protected]@H](C1=CC=C(C2=CC=C(S(=O)(C)=O)C=C2)C=C1)C(F)(F)F)C(NC3(C#N)CC3)=O


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    In Vitro

    In vitro activity: 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


    Kinase Assay: Odanacatib, also known as 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. Odanacatib selectively binds to and inhibits the activity of cathepsin K, which may result in a reduction in bone resorption, improvement of bone mineral density, and a reversal in osteoporotic changes. 


    Cell Assay: To assess cell survival, differentiated osteoclast (OC) at appr 7×104 cells/cm2 are re-seeded on bovine bone slices with or without 100 nM Odanacatib (ODN). Bone slices are fixed on days 2, 4, 6, and 12 with no media changes. Samples are stained for TRAP activity, and OC number.

    In VivoIn 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%). 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.
    Animal modelOvariectomized (OVX) rabbit model
    Formulation & DosageFormulated in diet; ≤9 µM/day; Oral gavage
    ReferencesBioorg Med Chem Lett. 2008 Feb 1;18(3):923-8; J Bone Miner Res. 2011 Feb;26(2):252-62


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     
    Odanacatib (MK-0822)
    Validation of the rabbit ovariectomized (OVX) model using estradiol and alendronate (ALN) treatment. J Bone Miner Res. 2011 Feb;26(2):252-62. 
     
    Odanacatib (MK-0822)
    Treatment with the cathepsin K inhibitors L-235 and odanacatib prevented bone loss in OVX rabbits. J Bone Miner Res. 2011 Feb;26(2):252-62. 
     
    Odanacatib (MK-0822)
    Effects of the cathepsin K inhibitors L-235 and odanacatib compared with ALN on bone formation in lumbar vertebrae cancellous bone and central femoral endocortical bone in OVX rabbits treated for 27-weeks. J Bone Miner Res. 2011 Feb;26(2):252-62. 
     
    Odanacatib (MK-0822)
    Correlation of ultimate load and BMC in the lumbar vertebrae and central femurs of OVX rabbits treated with ODN for 27 weeks.  J Bone Miner Res. 2011 Feb;26(2):252-62. 



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