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Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo.
| Molecular Weight | 540.63 |
| Formula | C27H32N4O6S |
| CAS Number | 362505-84-8 |
| Form | Solid |
| Solubility (25°C) | DMSO 40 mg/mL (ultrasonic and warming and heat to 60°C) |
| Storage | 4°C, protect from light, sealed |
| Related Cathepsin Products |
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| CAA-0225
CAA-0225 is a tissue protease L inhibitor that inhibits rat liver tissue protease L with a IC50 value of 1.9 nM. |
| 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. |
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