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Odanacatib

Cat. No. M1985

Odanacatib Structure

Synonym: MK-0822

Size Price Availability Quantity
5mg USD 100 In stock
10mg USD 170 In stock
50mg USD 480 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Odanacatib (MK-0822) is a selective and reversible inhibitor of cathepsin K (CatK). The cathepsin K inhibitor odanacatib (MK-0822) was shown to increase bone mineral density (BMD) and maintained normal bone strength at the spine in ovariectomized (OVX) rhesus monkeys. Odanacatib increased femoral neck (FN) BMD by 11% and 15% (p < 0.07) and ultimate load by 25% (p < 0.05) and 30% (p < 0.01) versus vehicle. Moreover, Odanacatib stimulated long-term FN and PF periosteal BFR by 3.5-fold and 6-fold with the 30 mg/kg dose versus vehicle, respectively. Odanacatib reduces bone turnover and increases bone mass in the lumbar spine of skeletally mature ovariectomized rhesus monkeys. Odanacatib was more selective than the published Cat K inhibitors balicatib and relacatib. Odanacatib (MK 0822) is currently in Phase II clinical trials.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 525.56
Formula C25H27F4N3O3S
CAS Number 603139-19-1
Purity >99%
Solubility DMSO 100 mg/mL
Storage at -20°C
References

Odanacatib treatment increases hip bone mass and cortical thickness by preserving endocortical bone formation and stimulating periosteal bone formation in the ovariectomized adult rhesus monkey.
Cusick T, et al. J Bone Miner Res. 2012 Mar;27(3):524-37. PMID: 22113921.

Odanacatib in the treatment of postmenopausal women with low bone mineral density: three-year continued therapy and resolution of effect.
Eisman JA, et al. J Bone Miner Res. 2011 Feb;26(2):242-51. PMID: 20740685.

The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Gauthier JY, et al. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. PMID: 18226527.

Related Cathepsin Products
UK-371804

UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).

Balicatib

Balicatib is a potent and selective inhibitor of cathepsin K; 10-100-fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Odanacatib, MK-0822 supplier, Cathepsin, inhibitors

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