230954-09-3

Name	CP-544439
CAS	230954-09-3
Molecular Formula	C18H19FN2O6S
MDL Number	MFCD34567141
Molecular Weight	410.42
MOL File	230954-09-3.mol

Synonyms

CP-544439 UNII-516DO4KL5R CP 544439,CP544439 2H-Pyran-4-carboxamide, 4-[[[4-(4-fluorophenoxy)phenyl]sulfonyl]amino]tetrahydro-N-hydroxy-

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Hazard Information

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

Supplier

Shanghai Yifei Biotechnology Co. , Ltd.

Telephone021-65675885 18964387627

Websitehttp://www.efebio.com

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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