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MK-0822

Names

[ CAS No. ]:
603139-12-4

[ Name ]:
MK-0822

[Synonym ]:
N1-(cyanomethyl)-N2{(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)-1,1'-biphenyl-4-yl]ethyl}-L-leucinamide
(S)-4-Methyl-2-[(S)-2,2,2-trifluoro-1-(4'-methanesulfonyl-biphenyl-4-yl)-ethylamino]-pentanoic acid cyanomethyl-amide
N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)-1,1'-biphenyl-4-yl]ethyl}-L-leucinamide
L-873724
N1-(cyanomethyl)-N2-{(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)-1,1'-biphenyl-4-yl]ethyl}-L-leucinamide
MK-0822

Biological Activity

[Description]:

L-873724 is a potent, orally bioavailable, selective and reversible[2] non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively[1]. L-873724 also exhibits an IC50 of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption[2].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Cathepsin
Research Areas >> Metabolic Disease

[Target]

IC50: 0.2 nM (Cathepsin K), 178 nM (Cathepsin S), 264 nM (Cathepsin B), 5239 nM (Cathepsin B)[1], 0.5 nM (Rabbit cathepsin K)[2]


[In Vitro]

L-873724 (Compound 22) is a potent and selective non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively. L-873724 also shows IC50s of 95, 1221 and 4807 nM for Ramos cathepsin S, Hep G2 cathepsin L, Hep G2 cathepsin B[1]. L-873724 exhibits an IC50 of 0.5 nM for rabbit cathepsin K[2].

[In Vivo]

L-873724 is orally bioavailable, non-lysosomotropic, and efficacious in the rhesus monkey bone resorption model[1].

[References]

[1]. Li CS, et al. Identification of a potent and selective non-basic cathepsin K inhibitor. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1985-9.

[2]. Zhuo Y, et al. Inhibition of bone resorption by the cathepsin K inhibitor odanacatib is fully reversible. Bone. 2014 Oct;67:269-80.


[Related Small Molecules]

Leupeptin hemisulfate salt | E-64 | PMSF | CA-074 methyl ester | LY 3000328 | Odanacatib(MK-0822) | CA 074 TFA | VBY-825 | Balicatib | Cysteine Protease inhibitor | Papain | Cathepsin Inhibitor 2 | E-64c | MIV-247

Chemical & Physical Properties

[ Molecular Formula ]:
C23H26F3N3O3S

[ Molecular Weight ]:
481.53100

[ Exact Mass ]:
481.16500

[ PSA ]:
107.44000

[ LogP ]:
5.86718

Related Compounds