Relacatib

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[1][2].

Product Specifications

CAS Number

[362505-84-8]

Product Name Alternative

SB-462795

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Cathepsin

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Cancer; Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/relacatib.html

Purity

99.99

Solubility

DMSO : 40 mg/mL (ultrasonic; warming; heat to 80°C)

Smiles

O=C(C1=CC2=CC=CC=C2O1)N[C@H](C(N[C@@H]3C(CN(S(=O)(C4=NC=CC=C4)=O)[C@H](C)CC3)=O)=O)CC(C)C

Molecular Formula

C27H32N4O6S

Molecular Weight

540.63

Precautions

H302, H315, H319, H335

References & Citations

[1]Dennis S Yamashita, et al. Structure Activity Relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one Cathepsin K Inhibitors.J Med Chem|[2]S Kumar, et al.A Highly Potent Inhibitor of Cathepsin K (Relacatib) Reduces Biomarkers of Bone Resorption Both in Vitro and in an Acute Model of Elevated Bone Turnover in Vivo in Monkeys.Bone. 2007 Jan;40 (1) :122-31.