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Odanacatib (CAS 603139-19-1)

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Alternate Names:
Odanacatib is also known as MK-0822.
Application:
Odanacatib is a neutral cathepsin K inhibitor with anti-osteoporotic and anti-resorptive activities.
CAS Number:
603139-19-1
Purity:
≥98%
Molecular Weight:
525.59
Molecular Formula:
C25H27F4N3O3S
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Odanacatib, a powerful and specific inhibitor of cathepsin K, effectively inhibits the enzymatic activity of cathepsin K with high potency (IC50s = 0.2 and 1 nM for human and rabbit enzymes, respectively). Cathepsin K is a protease responsible for osteoclastic bone resorption. Notably, odanacatib exhibits remarkable selectivity for cathepsin K over cathepsins B, L, and S. When formulated, odanacatib effectively decreases bone resorption while causing only modest reductions in bone formation. Consequently, this leads to an increase in bone mineral density.


Odanacatib (CAS 603139-19-1) References

  1. Pharmacokinetics and metabolism in rats, dogs, and monkeys of the cathepsin k inhibitor odanacatib: demethylation of a methylsulfonyl moiety as a major metabolic pathway.  |  Kassahun, K., et al. 2011. Drug Metab Dispos. 39: 1079-87. PMID: 21422190
  2. Osteoporosis: now and the future.  |  Rachner, TD., et al. 2011. Lancet. 377: 1276-87. PMID: 21450337
  3. Odanacatib reduces bone turnover and increases bone mass in the lumbar spine of skeletally mature ovariectomized rhesus monkeys.  |  Masarachia, PJ., et al. 2012. J Bone Miner Res. 27: 509-23. PMID: 22113859
  4. 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. 2012. J Bone Miner Res. 27: 524-37. PMID: 22113921
  5. Effects of Odanacatib on bone mineralization density distribution in thoracic spine and femora of ovariectomized adult rhesus monkeys: a quantitative backscattered electron imaging study.  |  Fratzl-Zelman, N., et al. 2013. Calcif Tissue Int. 92: 261-9. PMID: 23179105
  6. The bone resorption inhibitors odanacatib and alendronate affect post-osteoclastic events differently in ovariectomized rabbits.  |  Jensen, PR., et al. 2014. Calcif Tissue Int. 94: 212-22. PMID: 24085265
  7. Development and validation of an RP-HPLC method for the quantitation of odanacatib in rat and human plasma and its application to a pharmacokinetic study.  |  Police, A., et al. 2015. Biomed Chromatogr. 29: 1664-9. PMID: 25914381
  8. Odanacatib increases mineralized callus during fracture healing in a rabbit ulnar osteotomy model.  |  Pennypacker, BL., et al. 2016. J Orthop Res. 34: 72-80. PMID: 26178170
  9. Odanacatib Restores Trabecular Bone of Skeletally Mature Female Rabbits With Osteopenia but Induces Brittleness of Cortical Bone: A Comparative Study of the Investigational Drug With PTH, Estrogen, and Alendronate.  |  Khan, MP., et al. 2016. J Bone Miner Res. 31: 615-29. PMID: 26391310
  10. Effects of Long-Term Odanacatib Treatment on Bone Gene Expression in Ovariectomized Adult Rhesus Monkeys: Differentiation From Alendronate.  |  Muise, ES., et al. 2016. J Bone Miner Res. 31: 839-51. PMID: 26587671
  11. Odanacatib, effects of 16-month treatment and discontinuation of therapy on bone mass, turnover and strength in the ovariectomized rabbit model of osteopenia.  |  Duong, LT., et al. 2016. Bone. 93: 86-96. PMID: 27639811
  12. Effects of odanacatib on bone matrix mineralization in rhesus monkeys are similar to those of alendronate.  |  Misof, BM., et al. 2016. Bone Rep. 5: 62-69. PMID: 28326348
  13. Long-term treatment with odanacatib maintains normal trabecular biomechanical properties in ovariectomized adult monkeys as demonstrated by micro-CT-based finite element analysis.  |  Cabal, A., et al. 2017. Bone Rep. 6: 26-33. PMID: 28377978
  14. Differing Effects of Parathyroid Hormone, Alendronate, and Odanacatib on Bone Formation and on the Mineralization Process in Intracortical and Endocortical Bone of Ovariectomized Rabbits.  |  Vrahnas, C., et al. 2018. Calcif Tissue Int. 103: 625-637. PMID: 30019315
  15. Exploration of effect of Odanacatib on inhibiting orthodontic recurrence in rats and on CatK and IGF-1 mRNA.  |  Ye, J., et al. 2019. Eur Rev Med Pharmacol Sci. 23: 3151-3158. PMID: 31081065

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Odanacatib, 5 mg

sc-364675
5 mg
$218.00

Odanacatib, 25 mg

sc-364675A
25 mg
$993.00

Odanacatib, 250 mg

sc-364675B
250 mg
$1982.00

Hi, I am going to use this drug to inhibit Cathepsin K in my cell of interest. Could you tell me how to make (reconstitute) stock soln? Is this soluble in water? or, DMSO? MeOH? Thank you for your help!

Asked by: Tatapi
Thank you for your question. Odanacatib (CAS 603139-19-1) sc-364675 is reported to be soluble in DMSO and slightly in Chloroform and Methanol. Sonication may be needed for the latter two solvents and solutions should be prepared fresh. Stock solutions in DMSO may be stored at +4 °C for short term storage or at -20 °C for long term storage. For further information, please contact our technical service directly.
Answered by: Technical Support Europe
Date published: 2020-10-05
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Rated 5 out of 5 by from Schultz et alSchultz et al. (PubMed ID 26344800) found that Odanacatib inhibited cathepsin K and reduced bone absorption while also preserving bone formation in women with postmenopausal osteoporosis. -SCBT Publication Review
Date published: 2015-05-27
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Odanacatib is rated 5.0 out of 5 by 1.
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