MK-0822

Modify Date: 2024-01-10 14:35:59

MK-0822 Structure
MK-0822 structure
Common Name MK-0822
CAS Number 603139-12-4 Molecular Weight 481.53100
Density N/A Boiling Point N/A
Molecular Formula C23H26F3N3O3S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of MK-0822


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].

 Names

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

 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
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.

 Chemical & Physical Properties

Molecular Formula C23H26F3N3O3S
Molecular Weight 481.53100
Exact Mass 481.16500
PSA 107.44000
LogP 5.86718

 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
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