Odanacatib (MK-0822) is a selective and reversible inhibitor of cathepsin K (CatK). The cathepsin K inhibitor odanacatib (MK-0822) was shown to increase bone mineral density (BMD) and maintained normal bone strength at the spine in ovariectomized (OVX) rhesus monkeys. Odanacatib increased femoral neck (FN) BMD by 11% and 15% (p < 0.07) and ultimate load by 25% (p < 0.05) and 30% (p < 0.01) versus vehicle. Moreover, Odanacatib stimulated long-term FN and PF periosteal BFR by 3.5-fold and 6-fold with the 30 mg/kg dose versus vehicle, respectively. Odanacatib reduces bone turnover and increases bone mass in the lumbar spine of skeletally mature ovariectomized rhesus monkeys. Odanacatib was more selective than the published Cat K inhibitors balicatib and relacatib. Odanacatib (MK 0822) is currently in Phase II clinical trials.
J Appl Oral Sci. 2023 May 8;31:e20220449.
Do matrix metalloproteinase and cathepsin K inhibitors work synergistically to reduce dentin erosion?
Odanacatib purchased from AbMole
| Molecular Weight | 525.56 |
| Formula | C25H27F4N3O3S |
| CAS Number | 603139-19-1 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Cathepsin Products |
|---|
| Z-Gly-Pro-Arg-AMC hydrochloride
Z-Gly-Pro-Arg-AMC hydrochloride a fluorescent trypsin and cathepsin K substrate. |
| N-CBZ-Phe-Arg-AMC
N-CBZ-Phe-Arg-AMC (Z-FR-AMC) is a cathepsin substrate used in assessment activity of lysosomal cathepsin enzymes. |
| Ac-Glu-Asp(EDANS)-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Gly-Lys(DABCYL)-Glu-NH2
Ac-Glu-Asp(EDANS)-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Gly-Lys(DABCYL)-Glu-NH2 is a cathepsin D substrate, that can be used for cathepsin D FRET assay. |
| (S, S)-Z-FA-FMK
(S,S)-Z-FA-FMK is a cell-permeable, irreversible cathepsin B inhibitor. |
| H-Pro-Thr-Glu-Phe-p-nitro-Phe-Arg-Leu-OH
H-Pro-Thr-Glu-Phe-p-nitro-Phe-Arg-Leu-OH is a water-soluble polypeptide that can serve as a substrate for cathepsin D, pepsin and pepsinogen. |
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