Odanacatib (MK-0822)

For research use only.

Catalog No.S1115

21 publications

Odanacatib (MK-0822) Chemical Structure

CAS No. 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.

Selleck's Odanacatib (MK-0822) has been cited by 21 publications

Purity & Quality Control

Choose Selective Cysteine Protease Inhibitors

Biological Activity

Description 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.
Features A potent, selective, and neutral cathepsin K inhibitor.
Cathepsin K (human) [1]
Cathepsin K (rabbit) [1]
0.2 nM 1 nM
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. [1] A recent study shows that Odanacatib results in reduction of Osteoclast (OC) resorption activity by interrupting intracellular vesicular trafficking. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ramos cells Ml3mSpVv[3Srb36gZZN{[Xl? NHXpPXlKdmirYnn0bY9vKG:oIHPheIhmeHOrbjDTJIlvKGi3bXHuJJJidW:|IHPlcIx{NCCLQ{WwQVAvODR3zszN MljIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh{Mk[1NlcoRjF6MkK2OVI4RC:jPh?=
stem cells MlTBSpVv[3Srb36gZZN{[Xl? MYm3JIRigXN? M{TOOGlvcGmkaYTpc44hd2Zib4P0[Y9kdGG|dH;n[Y5me2m|IHnuJIh2dWGwIHLvcoUhdWG{cn;3MYRmemm4ZXSgd5RmdSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gdIl1KG[xcn3heIlwdiCkeTDt[YF{fXKrbnegWHJCS1B3YjDhZ5Rqfmm2eTDh[pRmeiB5IHThfZMh[nliYn;u[UBVWkGSIHHzd4F6NCCLQ{WwQVAvOc7:TR?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl6NEiwPUc,OjJ7OES4NFk9N2F-
HepG2 M2DHWmZ2dmO2aX;uJIF{e2G7 MnrvTY5pcWKrdHnvckBw\iClYYTo[ZB{cW5iQjDpckBpfW2jbjDI[ZBIOiClZXzsd{whUUN3ME2xMlA2|ryP NWjXU4M1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiyNlY2OjdpPkG4NlI3PTJ5PD;hQi=>
B cells NEDuO4dHfW6ldHnvckBie3OjeR?= MlS2TY5pcWKrdHnvckBw\iCjboTp[4VvKHC{ZYPlcpRqdmdibX;1d4UhSiClZXzsd{whUUN3ME2xMlXPxE1? NYTSdlZPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiyNlY2OjdpPkG4NlI3PTJ5PD;hQi=>
HepG2 Mo\GSpVv[3Srb36gZZN{[Xl? Mnf5TY5pcWKrdHnvckBw\iClYYTo[ZB{cW5iTDDpckBpfW2jbjDI[ZBIOiClZXzsd{whUUN3ME20Mlg1O87:TR?= M{XWPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MkK2OVI4Lz5zOEKyOlUzPzxxYU6=
SJ-GBM2 NHzvRXVyUFSVIHHzd4F6 MXnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-

... Click to View More Cell Line Experimental Data

In vivo In 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. [1] 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%). [3] 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. [4]


Animal Research:[3]
- Collapse
  • Animal Models: Ovariectomized (OVX) rabbit model
  • Dosages: ≤9 µM/day
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (190.27 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+corn oil
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 525.56


CAS No. 603139-19-1
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)(CC(C(=O)NC1(CC1)C#N)NC(C2=CC=C(C=C2)C3=CC=C(C=C3)S(=O)(=O)C)C(F)(F)F)F

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01803607 Terminated Drug: odanacatib|Other: placebo to odanacatib Osteoporosis Merck Sharp & Dohme Corp. March 14 2013 Phase 3
NCT01630616 Terminated Drug: Odanacatib|Drug: Placebo Osteoporosis Merck Sharp & Dohme Corp. March 12 2013 Phase 1
NCT01512693 Completed Drug: MK-0822 Hepatic Insufficiency Merck Sharp & Dohme Corp. February 23 2012 Phase 1
NCT01512667 Completed Drug: MK-0822 Renal Insufficiency Merck Sharp & Dohme Corp. January 17 2012 Phase 1
NCT01068262 Completed Drug: Odanacatib|Drug: Comparator: Placebo Osteoporosis Merck Sharp & Dohme Corp. December 8 2009 Phase 1
NCT00691899 Withdrawn Drug: odanacatib|Drug: placebo (unspecified) Prostate Cancer Merck Sharp & Dohme Corp. September 2008 Phase 3

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID