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Relacatib

CAT: 0804-HY-10294-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-10294-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, protect from light, stored under nitrogen)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
Cathepsin K; Cathepsin L

Alternative Products

CatalogName
MBS5800705Relacatib

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