CP-544439
- CAS No.
- 230954-09-3
- Chemical Name:
- CP-544439
- Synonyms
- CP-544439;UNII-516DO4KL5R;CP 544439,CP544439;2H-Pyran-4-carboxamide, 4-[[[4-(4-fluorophenoxy)phenyl]sulfonyl]amino]tetrahydro-N-hydroxy-
- CBNumber:
- CB34919684
- Molecular Formula:
- C18H19FN2O6S
- Molecular Weight:
- 410.42
- MDL Number:
- MFCD34567141
- MOL File:
- 230954-09-3.mol
FDA UNII | 516DO4KL5R |
---|
CP-544439 Chemical Properties,Uses,Production
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
CP-544439 Preparation Products And Raw materials
Raw materials
Preparation Products
CP-544439 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32268 | 58 |
TargetMol Chemicals Inc. | support@targetmol.com | United States | 38663 | 58 | |
Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11973 | 58 |
TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 19965 | 58 |
Supplier | Advantage |
---|---|
TargetMol Chemicals Inc. | 58 |
TargetMol Chemicals Inc. | 58 |
Shanghai Yifei Biotechnology Co. , Ltd. | 58 |
TargetMol Chemicals Inc. | 58 |