1. Metabolic Enzyme/Protease
  2. Cathepsin

Odanacatib (Synonyms: MK-0822; MK 0822; MK0822)

Cat. No.: HY-10042 Purity: 99.50%
Handling Instructions

Odanacatib is a potent, selective, and neutral inhibitor of cathepsin K (human/rabbit) with IC50 of 0.2 nM/1 nM, and demonstrates high selectivity versus off-target cathepsin B, L, S.

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Odanacatib Chemical Structure

Odanacatib Chemical Structure

CAS No. : 603139-19-1

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Description

Odanacatib is a potent, selective, and neutral inhibitor of cathepsin K (human/rabbit) with IC50 of 0.2 nM/1 nM, and demonstrates high selectivity versus off-target cathepsin B, L, S.

IC50 & Target

IC50: 0.2 nM (Human Cathepsin K), 1 nM (Rabbit Cathepsin K)

In Vitro

Odanacatib is a weak inhibitor of antigen presentation, measured in a mouse B cell line (IC50=1.5±0.4 μM), compared to the Cat S inhibitor LHVS (IC50=0.001 μM) in the same assay. Odanacatib also shows weak inhibition of the processing of the MHC II invariant chain protein Iip10 in mouse splenocytes compared to LHVS (minimum inhibitory concentration 1-10 μM versus 0.01 μM, respectively)[1]. Odanacatib reduces resorption activity as measured by CTx release (IC50=9.4 nM) or resorption area (IC50=6.5 nM), but has no impact on OC activation. Odanacatib dose-dependently reduces CTx release with an IC50=9.4±1.0 nM. Odanacatib treated OC accumulates labeled degraded bone matrix proteins in CatK containing vesicles[2].

In Vivo

Odanacatib (30 mg/kg, orally, once daily) persistently suppresses bone resorption markers and serum bone formation markers versus vehicle-treated OVX monkeys. Odanacatib displays compartment-specific effects on trabecular versus cortical bone formation, with treatment resulting in marked increases in periosteal bone formation and cortical thickness in ovariectomized monkeys whereas trabecular bone formation is reduced[3].

Clinical Trial
Sponsor Condition Start Date Phase
Merck & Co Inc Postmenopausal osteoporosis 2013-03-31 Phase 3
Merck & Co Inc Osteoporosis 2012-05-31 Phase 3
Merck & Co Inc Osteoporosis 2010-07-31 Phase 3
Merck & Co Inc Hormone refractory prostate cancer 2008-06-04 Phase 3
Merck & Co Inc Breast tumor 2008-06-04 Phase 3
References
M.Wt

525.56

Formula

C₂₅H₂₇F₄N₃O₃S

CAS No.

603139-19-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

Purity: 99.50%

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Odanacatib
Cat. No.:
HY-10042
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