Odanacatib (MK-0822)

Catalog No.S1115

For research use only.

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.

Odanacatib (MK-0822) Chemical Structure

CAS No. 603139-19-1

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.
Targets
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 MoLSSpVv[3Srb36gZZN{[Xl? M{f4NmlvcGmkaYTpc44hd2ZiY3H0bIVxe2mwIGOgbY4hcHWvYX6gdoFud3NiY3XscJMtKEmFNUC9NE4xPDYQvF2= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDJ{NkWyO{c,OTh{Mk[1Nlc9N2F-
stem cells M3y4RmZ2dmO2aX;uJIF{e2G7 NF;Rd3U4KGSjeYO= NV7FSXB2UW6qaXLpeIlwdiCxZjDvd5Rmd2OuYYP0c4dmdmW|aYOgbY4hcHWvYX6gZo9v\SCvYYLyc5cu\GW{aY\l[EB{fGWvIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBxcXRiZn;ycYF1cW:wIHL5JI1m[XO3cnnu[{BVWkGFUEXiJIFkfGm4aYT5JIFnfGW{IEeg[IF6eyCkeTDic45mKFSUQWCgZZN{[XluIFnDOVA:OC5zzszN MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl6NEiwPUc,OjJ7OES4NFk9N2F-
HepG2 MXnGeY5kfGmxbjDhd5NigQ>? NFP2SlZKdmirYnn0bY9vKG:oIHPheIhmeHOrbjDCJIlvKGi3bXHuJGhmeEd{IHPlcIx{NCCLQ{WwQVEvODYQvF2= NU\sbmF{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiyNlY2OjdpPkG4NlI3PTJ5PD;hQi=>
B cells MornSpVv[3Srb36gZZN{[Xl? NY\RVWxiUW6qaXLpeIlwdiCxZjDhcpRq\2WwIIDy[ZNmdnSrbnegcY92e2ViQjDj[YxteyxiSVO1NF0yNjYQvF2= NEXCRpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEKyOlUzPyd-MUiyNlY2Ojd:L3G+
HepG2 NXjXOI96TnWwY4Tpc44h[XO|YYm= NUH3dnpWUW6qaXLpeIlwdiCxZjDjZZRp\XC|aX6gUEBqdiCqdX3hckBJ\XCJMjDj[YxteyxiSVO1NF01Njh2M988US=> MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDJ{NkWyO{c,OTh{Mk[1Nlc9N2F-
SJ-GBM2 NYPt[45WeUiWUzDhd5NigQ>? M3H5dJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz NX;MTIhJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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]

Protocol (from reference)

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

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.

5mg/mL

Chemical Information

Molecular Weight 525.56
Formula

C25H27F4N3O3S

CAS No. 603139-19-1
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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.

Handling Instructions

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