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MedKoo product information:
Relacatib
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MedKoo Code#: 202440
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Name:
Relacatib
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CAS#:
362505-84-8
Synonym: SB-462795。,
GSK-462795；D06634。2-Benzofurancarboxamide,
N-[(1S)-1-[[[(4S,7R)-hexahydro-7-methyl-3-oxo-1-(2-pyridinylsulfonyl)-1H-azepin-4-yl]amino]carbonyl]-3-methylbutyl]-
IUPAC/Chemical name:
N-((S)-4-methyl-1-(((4S,7R)-7-methyl-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)amino)-1-oxopentan-2-yl)benzofuran-2-carboxamide.
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Chemical structure: |
Theoretical analysis
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Chemical Formula: C27H32N4O6S
Exact Mass: 540.20426
Molecular Weight: 540.63
m/z: 540.20426 (100.0%), 541.20761 (29.2%),
542.20005 (4.5%), 542.21097 (4.1%), 541.20129 (1.5%), 543.20341
(1.3%), 542.20850 (1.2%)
Elemental Analysis: C, 59.98; H, 5.97;
N, 10.36; O, 17.76; S, 5.93
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Availability and price:
This agent is not in stock, which may be available through custom synthesis. To inquire quotation and lead time or to ask questions, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
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Quality control
data:
Product will be shipped with
supporting analytical data.
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Information about this agent
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Relacatib (SB-462795) is a
high-potency inhibitor of cathepsin K with demonstrated antiresorptive
activity in normal and ovariectomized monkeys. Studies in ovariectomized
monkeys also demonstrated a greater stimulatory effect on cortical bone
compared to alendronate, with significant improvements in bone mineral
density and bone mineral content compared with vehicle-treated controls.
Studies in monkeys indicate site-specific differences between
alendronate and relacatib which may translate into differential
efficacy. (from drugs
of the future)
Current developer:
GlaxoSmithKline.
1: Stroup GB, Kumar S, Jerome CP. Treatment
with a potent cathepsin K inhibitor preserves cortical and trabecular
bone mass in ovariectomized monkeys. Calcif Tissue Int. 2009
Oct;85(4):344-55. Epub 2009 Sep 10. PubMed PMID: 19763376.
2: Kadono Y, Tanaka S. [Prevention of joint destruction by osteoclast-targeting
therapy in search of new tools, such as OPG or cathepsin K inhibitor].
Clin Calcium. 2009 Mar;19(3):387-93. Review. Japanese. PubMed PMID:
19252249.
3: Le Gall C, Bonnelye E, Clézardin P. Cathepsin K inhibitors as
treatment of bone metastasis. Curr Opin Support Palliat Care. 2008
Sep;2(3):218-22. Review. PubMed PMID: 18685424.
4: Kamiya N, Suzuki H, Kawamura K, Imamoto T, Ichikawa T. [Bony lesion
with prostate cancer]. Clin Calcium. 2008 Apr;18(4):431-7. Review.
Japanese. PubMed PMID: 18379023.
5: Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong le T,
Falgueyret JP, Kimmel DB, Lamontagne S, Léger S, LeRiche T, Li CS, Massé
F, McKay DJ, Nicoll-Griffith DA, Oballa RM, Palmer JT, Percival MD,
Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong
VL, Venuti MC, Wesolowski G, Young RN, Zamboni R, Black WC. The
discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. Epub 2008 Jan 15. PubMed
PMID: 18226527.
6: Kumar S, Dare L, Vasko-Moser JA, James IE, Blake SM, Rickard DJ,
Hwang SM, Tomaszek T, Yamashita DS, Marquis RW, Oh H, Jeong JU, Veber
DF, Gowen M, Lark MW, Stroup G. 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. Epub 2006 Sep 7. PubMed PMID: 16962401.
7: Yamashita DS, Marquis RW, Xie R, Nidamarthy SD, Oh HJ, Jeong JU,
Erhard KF, Ward KW, Roethke TJ, Smith BR, Cheng HY, Geng X, Lin F, Offen
PH, Wang B, Nevins N, Head MS, Haltiwanger RC, Narducci Sarjeant AA,
Liable-Sands LM, Zhao B, Smith WW, Janson CA, Gao E, Tomaszek T,
McQueney M, James IE, Gress CJ, Zembryki DL, Lark MW, Veber DF.
Structure activity relationships of 5-, 6-, and 7-methyl-substituted
azepan-3-one cathepsin K inhibitors. J Med Chem. 2006 Mar
9;49(5):1597-612. PubMed PMID: 16509577.
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