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Relacatib
$1,150 – $3,600
Products Details
Product Description
– 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].
Web ID
– HY-10294
Storage Temperature
– 4°C (Powder, protect from light, stored under nitrogen)
Shipping
– Room Temperature
Applications
– Metabolism-protein/nucleotide metabolism
Molecular Formula
– C27H32N4O6S
References
– [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.
CAS Number
– 362505-84-8
Molecular Weight
– 540.63
Compound Purity
– 99.99
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
Clinical Information
– Phase 1
Research Area
– Cancer; Metabolic Disease
Solubility
– DMSO : 40 mg/mL (ultrasonic;warming;heat to 80°C)
Target
– Cathepsin
Isoform
– Cathepsin K;Cathepsin L
Pathway
– Metabolic Enzyme/Protease
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
