| Identification | Back Directory | [Name]
CP-544439 | [CAS]
230954-09-3 | [Synonyms]
CP-544439
UNII-516DO4KL5R
CP 544439,CP544439
2H-Pyran-4-carboxamide, 4-[[[4-(4-fluorophenoxy)phenyl]sulfonyl]amino]tetrahydro-N-hydroxy- | [Molecular Formula]
C18H19FN2O6S | [MDL Number]
MFCD34567141 | [MOL File]
230954-09-3.mol | [Molecular Weight]
410.42 |
| Hazard Information | Back Directory | [Uses]
CP-544439 is a potent and orally active matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 0.75 nM[1][2]. | [in vivo]
In vivo studies using a hamster model, in which the cartilage collagen degradation was induced by intra-articular injection of recombinant human MMP-13, demonstrated that oral administration of CP-544439 inhibits degradation of the cartilage collagen with an ED50 of 14 mg/kg and efficacious plasma concentrations ranging from 0.5 to 1.0 g/ml[1]. | [IC 50]
MMP-13: 0.75 nM (IC50); MMP-12: 0.24 nM (IC50); MMP-1: 420 nM (IC50); MMP-2: 1.6 nM (IC50); MMP-3: 16 nM (IC50); MMP-8: 1.4 nM (IC50); MMP-9: 12 nM (IC50); MMP-14: 7.4 nM (IC50) | [References]
[1] Dalvie D, et al. Metabolism distribution and excretion of a matrix metalloproteinase-13 inhibitor, 4-[4-(4-fluorophenoxy)-benzenesulfonylamino]tetrahydropyran-4-carboxylic acid hydroxyamide (CP-544439), in rats and dogs: assessment of the metabolic profil DOI:10.1124/dmd.108.022566
[2] Reiter LA, et al. Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1. Bioorg Med Chem Lett. 2004;14(13):3389-3395. DOI:10.1016/j.bmcl.2004.04.083 |
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