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Gamma Secretase

Odanacatib (MK-0822) (603139-19-1)

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.

Not Intended for Therapeutic Use. For research use only.

CAS: 603139-19-1 Category

Odanacatib (MK-0822) (603139-19-1) Description:

Odanacatib, also known as 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.

Odanacatib (MK-0822) (603139-19-1) Specifications:

Product Name Odanacatib (MK0822)
Synonyms MK0822; MK-0822; MK 0822; Odanacatib .
Chemical Names (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
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 603139-19-1
Molecular Formula C25H27F4N3O3S
Molecular Weight 525.56
Monoisotopic Mass 525.171 g/mol
MDL number MFCD11042419
InChIKey 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 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
Form Powder
Color white
Solubility  Soluble in DMSO, not in water
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly.
Handling Protect from air and light
Application Odanacatib (MK-0822) is a potent and selective inhibitor of cathepsin K, with an IC50 of 0.2 nM for human cathepsin K.

 


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RIDADR NONH for all modes of transport

References:

  • 1: Chapurlat RD. Treatment of postmenopausal osteoporosis with odanacatib. Expert Opin Pharmacother. 2014 Jan 24. [Epub ahead of print] PubMed PMID: 24456412.
  • 2: Odanacatib, a cathepsin K inhibitor, superior to alendronate. Bonekey Rep. 2013 Sep 4;2:426. doi: 10.1038/bonekey.2013.160. eCollection 2013. PubMed PMID: 24422127; PubMed Central PMCID: PMC3789222.
  • 3: Retraction notice: Odanacatib for the treatment of postmenopausal osteoporosis. Expert Opin Pharmacother. 2014 Jan;15(1):151. doi: 10.1517/14656566.2014.868399. Epub 2013 Nov 30. PubMed PMID: 24289716.
  • 4: Anderson MS, Gendrano IN, Liu C, Jeffers S, Mahon C, Mehta A, Mostoller K, Zajic S, Morris D, Lee J, Stoch SA. Odanacatib, a selective cathepsin K inhibitor, demonstrates comparable pharmacodynamics and pharmacokinetics in older men and postmenopausal women. J Clin Endocrinol Metab. 2013 Dec 20:jc20131688. [Epub ahead of print] PubMed PMID: 24276460.
  • 5: Chapurlat RD. Odanacatib for the treatment of postmenopausal osteoporosis. Expert Opin Pharmacother. 2014 Jan;15(1):97-102. doi: 10.1517/14656566.2014.853038. Epub 2013 Oct 25. Retraction in: Expert Opin Pharmacother. 2014 Jan;15(1):151. PubMed PMID: 24156249.

1 review for Odanacatib (MK-0822) (603139-19-1)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The Odanacatib (MK-0822) (603139-19-1) is high purity,also customer service is pretty nice !gotta try!!

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