L 873724

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

L 873724 是一种有效的选择性非碱性组织蛋白酶 K 抑制剂，IC50 为 0.2 nM。

L 873724 is a potent and selective non-basic cathepsin K inhibitor with IC50 of 0.2 nM, shows no significant potency against Cat B, L, and S (IC50= 5239, 264, and 178 nM); demonstrates excellent pharmacokinetics and efficacy in an ovariectomized (OVX) rhesus monkey model.Osteoporosis Phase 1 Discontinued.

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. L-873724 exhibits an IC50 of 0.5 nM for rabbit cathepsin K.

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

L873724

Metabolic Enzyme/Protease

Cathepsin

Cathepsin

Metabolic Disease

Osteoporosis

603139-12-4

481.534

C23H26F3N3O3S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (207.67 mM)

CC(C)C[C@H](N[C@@H](C1=CC=C(C2=CC=C(S(=O)(C)=O)C=C2)C=C1)C(F)(F)F)C(NCC#N)=O

(2S)-N-(cyanomethyl)-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide

(-20℃)

With Ice Pack

≥ 2 years