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Home - Products - Metabolic Enzyme/Protease - Cathepsin - L 873724

L 873724

CAS No. 603139-12-4

L 873724( L873724 )

Catalog No. M15251 CAS No. 603139-12-4

L 873724 is a potent and selective non-basic cathepsin K inhibitor with IC50 of 0.2 nM.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    L 873724
  • Note
    Research use only, not for human use.
  • Brief Description
    L 873724 is a potent and selective non-basic cathepsin K inhibitor with IC50 of 0.2 nM.
  • Description
    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.
  • 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. L-873724 exhibits an IC50 of 0.5 nM for rabbit cathepsin K.
  • In Vivo
    L-873724 is orally bioavailable, non-lysosomotropic, and efficacious in the rhesus monkey bone resorption model.
  • Synonyms
    L873724
  • Pathway
    Metabolic Enzyme/Protease
  • Target
    Cathepsin
  • Recptor
    Cathepsin
  • Research Area
    Metabolic Disease
  • Indication
    Osteoporosis

Chemical Information

  • CAS Number
    603139-12-4
  • Formula Weight
    481.534
  • Molecular Formula
    C23H26F3N3O3S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (207.67 mM)
  • SMILES
    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
  • Chemical Name
    (2S)-N-(cyanomethyl)-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Li CS, et al. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1985-9. 2. Desmarais S, et al. Mol Pharmacol. 2008 Jan;73(1):147-56. 3. Pennypacker BL, et al. BMC Musculoskelet Disord. 2013 Dec 9;14:344.
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