1. Metabolic Enzyme/Protease
  2. Cathepsin

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

Cat. No.: HY-10042 Purity: 99.80%
Data Sheet SDS 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

Size Price Stock Quantity
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
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500 mg   Get quote  

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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]. The bone volume/total volume (BV/TV) and bone mineral density (BMD) of the OVX + ODN-h group is significantly higher than that of the OVX + Veh group (p < 0.05). The expressions of Runx2, Collagen-1, BSP, Osterix, OPN and SPP1 are significantly lower in the OVX + ODN-h group than in the OVX + Veh group (p < 0.01). Compared with the OVX + Veh group, the expressions of Collagen-I, BSP, Osterix, OPN and ALP reduce in the OVX + ODN-l group, but are upregulated in the OVX + ODN-h group[4].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01512693 Merck Sharp & Dohme Corp. Hepatic Insufficiency February 2012 Phase 1
NCT01512667 Merck Sharp & Dohme Corp. Renal Insufficiency January 2012 Phase 1
NCT00770159 Merck Sharp & Dohme Corp. Osteoporosis November 2004 Phase 1
NCT00397683 Merck Sharp & Dohme Corp. Osteoarthritis October 2006 Phase 2
NCT00112437 Merck Sharp & Dohme Corp. Osteoporosis June 2005 Phase 2
NCT00242476 Merck Sharp & Dohme Corp. Vitamin D Deficiency September 2005 Phase 2
NCT01068262 Merck Sharp & Dohme Corp. Osteoporosis December 8, 2009 Phase 1
NCT00769418 Merck Sharp & Dohme Corp. Osteoporosis September 2004 Phase 1
NCT01803607 Merck Sharp & Dohme Corp. Osteoporosis March 2013 Phase 3
NCT00863525 Merck Sharp & Dohme Corp. Osteoporosis November 2004 Phase 1
NCT00691899 Merck Sharp & Dohme Corp. Prostate Cancer September 2008 Phase 3
NCT01120600 Merck Sharp & Dohme Corp. Osteoporosis June 2010 Phase 3
NCT01630616 Merck Sharp & Dohme Corp. Osteoporosis March 2013 Phase 1
NCT00692458 Merck Sharp & Dohme Corp. Breast Cancer September 2008 Phase 3
NCT00729183 Merck Sharp & Dohme Corp. Osteoporosis October 2008 Phase 3
NCT00529373 Merck Sharp & Dohme Corp. Postmenopausal Osteoporosis September 2007 Phase 3
NCT00620113 Merck Sharp & Dohme Corp. Osteoporosis Postmenopausal December 2007 Phase 2
NCT00885170 Merck Sharp & Dohme Corp. Osteoporosis April 2009 Phase 2
NCT01552122 Merck Sharp & Dohme Corp. Osteoporosis|Postmenopausal Osteoporosis May 2012 Phase 3
NCT00863590 Merck Sharp & Dohme Corp. Osteoporosis June 2004 Phase 1
NCT00399802 Merck Sharp & Dohme Corp. Breast Cancer|Metastatic Bone Disease November 2006 Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 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
Animal Administration
[4]

Odanacatib is added in 0.5% sodium carboxymethyl cellulose.

Sixteen, 8-month-old, female Sprague-Dawley (SD) rats (weight, 385 ± 55 g) are given water and soft diet food ad libitum in a temperature-controlled environment with regular 12-h cycles of light and dark. The rats are randomised into 4 groups, with 4 rats in each group: sham group, OVX + Veh group, OVX + ODN-l group and OVX + ODN-h group. Following implant insertion, Odanacatib (ODN, 5 mg/mL) is administered to the OVX + ODN-l and OVX + ODN-h groups at concentrations of 1 mL/kg and 6 mL/kg, respectively, by gavaging once a day for 8 weeks. The OVX + Veh group is gavaged with 0.5% sodium carboxymethyl cellulose at a concentration of 6 mL/kg over the same duration. After the gavage administration, the rats of each group are sacrificed by injecting sodium pentobarbital intravenously. The implants are harvested and fixed in 10% buffered formalin together with the surrounding bone.

References
M.Wt

525.56

Formula

C₂₅H₂₇F₄N₃O₃S

CAS No.

603139-19-1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥25 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.80%

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Odanacatib
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