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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 |
|---|
| N-Ethylmaleimide
N-Ethylmaleimide (NEM) is a cysteine protease inhibitor. |
| Odanacatib
Odanacatib (MK-0822) is a potent and reversible covalent inhibitor of CathepsinK (CatK) with an IC50 of 0.2 nM/1 nM for human/rabbit cathepsin B, L, and S and is highly selective. |
| Balicatib
Balicatib is a potent and selective inhibitor of cathepsin K; 10-100-fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S. |
| Aloxistatin
Aloxistatin (E64d) is an irreversible and membrane-permeable cysteine protease inhibitor. |
| Cathepsin Inhibitor 1
Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively. |
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