603139-12-4

603139-12-4 structure

Name: MK-0822
Chemical Name: (2S)-4-methyl-2-[(1S)-2,2,2-trifluoro-1-(4'-methanesulfonyl-biphenyl-4-yl)ethylamino]-pentanoic acid cyanomethyl-amide
CAS Number: 603139-12-4
Molecular Formula: C₂₃H₂₆F₃N₃O₃S
Molecular Weight: 481.53100
Catalog: Signaling Pathways Metabolic Enzyme/Protease Cathepsin
Create Date: 2018-06-15 21:04:31
Modify Date: 2024-01-10 14:35:59
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].

Name	(2S)-4-methyl-2-[(1S)-2,2,2-trifluoro-1-(4'-methanesulfonyl-biphenyl-4-yl)ethylamino]-pentanoic acid cyanomethyl-amide
Synonyms	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

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.