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> Odanacatib [603139-19-1]

Odanacatib [603139-19-1]

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Odanacatib (MK-0822) is a potent and selective inhibitor of cathepsin K, with an IC50 of 0.2 nM for human cathepsin K.

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Odanacatib Estructura química

Odanacatib Estructura química

No. CAS : 603139-19-1

This product is a controlled substance and not for sale in your territory.

Based on 7 publication(s) in Google Scholar

Other Forms of Odanacatib:

  • Odanacatib-d4 Obtener un presupuesto

Ver todos los productos específicos de isoformas Cathepsin:

Ver todas las isoformas
Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S
Descripciòn

Odanacatib (MK-0822) is a potent and selective inhibitor of cathepsin K, with an IC50 of 0.2 nM for human cathepsin K.

IC50 & Target

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Odanacatib Related Antibodies
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?[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
Peso molecular

525.56

Fòrmula

C25H27F4N3O3S
No. CAS

603139-19-1
Appearance

Solid

Color

White to brown

SMILES

N#CC1(NC([C@@H](N[C@H](C(F)(F)F)C2=CC=C(C3=CC=C(S(=O)(C)=O)C=C3)C=C2)CC(C)(F)C)=O)CC1
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
In Vitro: 

DMSO : ≥ 25 mg/mL (47.57 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación

Purity: 99.82%

COA (254 KB) LCMS (264 KB)

Instrucciones de manejo (2659 KB)
Referencias

  • [1]. Jacques Yves Gauthier, et al. The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8.  [Content Brief]

    [2]. Leung P, et al. The effects of the cathepsin K inhibitor odanacatib on osteoclastic bone resorption and vesicular trafficking. Bone. 2011 Oct;49(4):623-635.  [Content Brief]

    [3]. Ng KW. Potential role of odanacatib in the treatment of osteoporosis. Clin Interv Aging. 2012;7:235-47.  [Content Brief]

    [4]. Yi C, et al. Inhibition of cathepsin K promotes osseointegration of titanium implants in ovariectomised rats. Sci Rep. 2017 Mar 17;7:44682.  [Content Brief]

Ensayo celular
[2]

To assess cell survival, differentiated osteoclast (OC) at appr 7×104 cells/cm2 are re-seeded on bovine bone slices with or without 100 nM Odanacatib (ODN). Bone slices are fixed on days 2, 4, 6, and 12 with no media changes. Samples are stained for TRAP activity, and OC number.

MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Administraciòn de animales
[4]

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.

MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias

  • [1]. Jacques Yves Gauthier, et al. The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8.  [Content Brief]

    [2]. Leung P, et al. The effects of the cathepsin K inhibitor odanacatib on osteoclastic bone resorption and vesicular trafficking. Bone. 2011 Oct;49(4):623-635.  [Content Brief]

    [3]. Ng KW. Potential role of odanacatib in the treatment of osteoporosis. Clin Interv Aging. 2012;7:235-47.  [Content Brief]

    [4]. Yi C, et al. Inhibition of cathepsin K promotes osseointegration of titanium implants in ovariectomised rats. Sci Rep. 2017 Mar 17;7:44682.  [Content Brief]

  • [1]. Jacques Yves Gauthier, et al. The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8.

    [2]. Leung P, et al. The effects of the cathepsin K inhibitor odanacatib on osteoclastic bone resorption and vesicular trafficking. Bone. 2011 Oct;49(4):623-635.

    [3]. Ng KW. Potential role of odanacatib in the treatment of osteoporosis. Clin Interv Aging. 2012;7:235-47.

    [4]. Yi C, et al. Inhibition of cathepsin K promotes osseointegration of titanium implants in ovariectomised rats. Sci Rep. 2017 Mar 17;7:44682.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9027 mL 9.5137 mL 19.0273 mL 47.5683 mL
5 mM 0.3805 mL 1.9027 mL 3.8055 mL 9.5137 mL
10 mM 0.1903 mL 0.9514 mL 1.9027 mL 4.7568 mL
15 mM 0.1268 mL 0.6342 mL 1.2685 mL 3.1712 mL
20 mM 0.0951 mL 0.4757 mL 0.9514 mL 2.3784 mL
25 mM 0.0761 mL 0.3805 mL 0.7611 mL 1.9027 mL
30 mM 0.0634 mL 0.3171 mL 0.6342 mL 1.5856 mL
40 mM 0.0476 mL 0.2378 mL 0.4757 mL 1.1892 mL
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Odanacatib Related Classifications

  • Metabolic Enzyme/Protease
  • Cathepsin
Help & FAQs

Keywords:

Odanacatib603139-19-1MK-0822MK0822MK 0822CathepsinInhibitorinhibitorinhibit

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