Successful, we will reply to you quickly.

OK

Please select the quantity.

OK

Your message is being sent, please wait.

Close

test

Close

Send mail failed, please send again!

Close

Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

Odanacatib

HY-10042

(MK-0822; MK 0822; MK0822)

Odanacatib

Odanacatib Chemical Structure

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.

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $116 In-stock
5 mg $100 In-stock
10 mg $160 In-stock
50 mg $400 In-stock
100 mg $600 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €114 In-stock
5 mg €98 In-stock
10 mg €157 In-stock
50 mg €392 In-stock
100 mg €588 In-stock
200 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

Bulk Inquiry

Inquiry Information
Product name: Odanacatib
Cat. No.: HY-10042

Odanacatib Data Sheet

  • View current batch:

    Purity: 98.27% ee.:98.96%

  • Pdf Version Network Version

    DataSheet

    Pdf Version Network Version

    MSDS

    Pdf Version

    COA

Related Compound Libraries

Biological Activity of Odanacatib

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.
IC50 value: 0.2 nM/1 nM(human/rabbi cathepsin K)
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. A recent study shows that Odanacatib results in reduction of Osteoclast (OC) resorption activity by interrupting intracellular vesicular trafficking.
in vivo: n 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%).

Protocol (Extracted from published papers and Only for reference)

More

Chemical Information

M.Wt 525.56 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C25H27F4N3O3S
CAS No 603139-19-1
Solvent & Solubility

DMSO ≥102mg/mL Water <1.2mg/mL Ethanol ≥2.9mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 1.9027 mL 9.5137 mL 19.0273 mL
5 mM 0.3805 mL 1.9027 mL 3.8055 mL
10 mM 0.1903 mL 0.9514 mL 1.9027 mL

Clinical Information of Odanacatib

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
Odanacatib Merck & Co Inc Postmenopausal osteoporosis 31-MAR-13 30-SEP-15 Phase 3 18-MAY-13
Merck & Co Inc Osteoporosis 31-JUL-10 31-JUL-13 Phase 3 15-NOV-13
Merck & Co Inc Hormone refractory prostate cancer 04-JUN-08 31-AUG-08 Phase 3 15-JUN-10
Merck & Co Inc Osteoporosis 31-MAY-12 28-FEB-15 Phase 3 11-SEP-13
Merck & Co Inc Breast tumor 04-JUN-08 31-AUG-08 Phase 3 19-DEC-08

References on Odanacatib

[1]. Jacques Yves Gauthier, Nathalie ChauretThe discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K Bioorganic & Medicinal Chemistry Letters Volume 18, Issue 3, 1 February 2008, Pages 923-928
Abstract
Odanacatib is a potent, selective, and neutral cathepsin K inhibitor which was developed to address the metabolic liabilities of the Cat K inhibitor L-873724. Substituting P1 and modifying the P2 side chain led to a metabolically robust inhibitor with a long half-life in preclinical species. Odanacatib was more selective in whole cell assays than the published Cat K inhibitors balicatib and relacatib. Evaluation in dermal fibroblast culture showed minimal intracellular collagen accumulation relative to less selective Cat K inhibitors....

[2]. Ng KW.Potential role of odanacatib in the treatment of osteoporosis.Clin Interv Aging. 2012;7:235-47. Epub 2012 Jul 12.

[3]. Langdahl B, Binkley N, Bone H, Gilchrist N, Resch H, Portales JR, Denker A, Lombardi A, De Tilleghem CL, Dasilva C, Rosenberg E, Leung A.Odanacatib in the treatment of postmenopausal women with low bone mineral density: 5 years of continued therapy in a phase 2 study.J Bone Miner Res. 2012 Jul 6.

[4]. Khosla S.Odanacatib: location and timing are everything.J Bone Miner Res. 2012 Mar;27(3):506-8.

[5]. Sun L, Forni S, Schwartz MS, Breidinger S, Woolf EJ.Quantitative determination of odanacatib in human plasma using liquid-liquid extraction followed by liquid chromatography-tandem mass spectrometry analysis.J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Feb 15;885-886:15-23. Epub 2011 Dec 13.

Inhibitor Kit

Related Cathepsin Products

  • Balicatib

    Balicatib(AAE-581) 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.

  • Cathepsin S inhibitor

    Cathepsin S inhibitor is a novel Cathepsin S inhibitor.

  • E-64

    E-64 is a natural, potent, and irreversible inhibitor of cysteine proteases; IC50 values for inhibiting cathepsins K, S, and L, in vitro, are 1.4, 4.1, and 2.5 nM, respectively.

  • Leupeptin hemisulfate

    Leupeptin hemisulfate is a reversible, competitive serine/cysteine protease inhibitor, which has been shown to inhibit cathepsins B, H, L, and S, calpain, and trypsin.

  • Pepstatin

    Pepstatin is a potent inhibitor of aspartyl proteases; inhibits the aspartic proteases cathepsin D, pepsin, and renin.

  • VBY-825

    VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.