Odanacatib

Synonyms: MK-0822

Odanacatib 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 Chemical Structure

Odanacatib Chemical Structure

CAS No. 603139-19-1

Purity & Quality Control

Odanacatib Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ramos cells Function assay Inhibition of cathepsin S in human ramos cells, IC50=0.045μM 18226527
stem cells Function assay 7 days Inhibition of osteoclastogenesis in human bone marrow-derived stem cells assessed as reduction of pit formation by measuring TRACP5b activity after 7 days by bone TRAP assay, IC50=0.1μM 22984809
HepG2 Function assay Inhibition of cathepsin B in human HepG2 cells, IC50=1.05μM 18226527
B cells Function assay Inhibition of antigen presenting mouse B cells, IC50=1.5μM 18226527
HepG2 Function assay Inhibition of cathepsin L in human HepG2 cells, IC50=4.843μM 18226527
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
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Biological Activity

Description Odanacatib 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 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]
In Vivo
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 Animal Models Ovariectomized (OVX) rabbit model
Dosages ≤9 µM/day
Administration Administered via p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01803607 Terminated
Osteoporosis
Merck Sharp & Dohme LLC
March 14 2013 Phase 3
NCT01630616 Terminated
Osteoporosis
Merck Sharp & Dohme LLC
March 12 2013 Phase 1
NCT01512693 Completed
Hepatic Insufficiency
Merck Sharp & Dohme LLC
February 23 2012 Phase 1
NCT01512667 Completed
Renal Insufficiency
Merck Sharp & Dohme LLC
January 17 2012 Phase 1
NCT01068262 Completed
Osteoporosis
Merck Sharp & Dohme LLC
December 8 2009 Phase 1
NCT00691899 Withdrawn
Prostate Cancer
Merck Sharp & Dohme LLC
September 2008 Phase 3

Chemical Information & Solubility

Molecular Weight 525.56 Formula

C25H27F4N3O3S

CAS No. 603139-19-1 SDF Download Odanacatib SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 105 mg/mL ( (199.78 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
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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.

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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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