L 006235

L 006235

Catalog Number:
L002369203APE
Mfr. No.:
APE-A4422
Price:
$555
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      • Overview
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          Background

          IC50: 0.25 nML-006235 is a potent and selective inhibitor of Cathepsin K.In vitro: After dilution of L-006235 to 0.05 nM, the cathepsin K enzyme activity was initially inhibited, but slowly recovered with a first-order rate constant of 0.023 s-1. The final steady-state enzyme activity was 80-90% that of control, suggesting the complete reversibility of the L-006235-cathepsin K complex. L-006235 was found to be not a substrate for the nitrilase activity of Cat K [1]. In vivo: L-006235 was orally bioavailable in rats, with a terminal half-life of over 3 h. L-006235 was orally dosed in ovariectomized rhesus monkeys once per day for 7 days. Results showed that collagen breakdown products were dose-dependently reduced by up to 76%. Plasma concentrations of L-006235 above the bone resorption IC50 after 24 h indicated a correlation between functional cellular and in vivo assays. These findings suggested that the inhibition of collagen breakdown by cathepsin K inhibitors, such as L-006235, might be useful in osteoporosis and other indications involving bone resorption [1]. Clinical trial: N/A

      • Properties
        • Alternative Name
          N-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
          CAS Number
          294623-49-7
          Molecular Formula
          C24H30N6O2S
          Molecular Weight
          466.6
          Appearance
          White solid
          Purity
          98.00%
          Solubility
          <46.66mg/ml in DMSO
          Storage
          Store at 4°C

          * For Research Use Only

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