Biological Activity
Broad spectrum MMP inhibitor. Displays high affinity for MMP-2, -3 and -13 (IC50 values are 4, 7 and 8 nM respectively) and exhibits > 750-fold selectivity over MMP-1, -7 and -9. Attenuates left ventricular remodelling and dysfunction in rat model of heart failure.
Compound Libraries
PD 166793 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 412.3 |
| Formula | C17H18BrNO4S |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 199850-67-4 |
| PubChem ID | 9887870 |
| InChI Key | GJOCABIDMCKCEG-INIZCTEOSA-N |
| Smiles | BrC1=CC=C(C2=CC=C(S(N[C@@H]([C@H](C)C)C(O)=O)(=O)=O)C=C2)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.23 | 100 | |
| ethanol | 41.23 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 412.3. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.43 mL | 12.13 mL | 24.25 mL |
| 5 mM | 0.49 mL | 2.43 mL | 4.85 mL |
| 10 mM | 0.24 mL | 1.21 mL | 2.43 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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References
References are publications that support the products' biological activity.
O'Brien et al (2000) Structure-activity relationships and pharmacokinetic analysis for a series of potent, systemically available Biphenylsulfonamide matrix metalloproteinase inhibitors. J.Med.Chem. 43 156 PMID: 10649971
Peterson et al (2001) Matrix metalloproteinase inhibition attenuates left ventricular remodeling and dysfunction in a rat model of progressive heart failure. Circulation 103 2303 PMID: 11342481
Chancey et al (2002) Effects of matrix metalloproteinase inhibition on ventricular remodeling due to volume overload. Circulation 105 1983 PMID: 11997287
Keywords: PD 166793, supplier, Broad, spectrum, MMP, inhibitors, inhibits, Matrixins, Matrix, Metalloproteinase, Metalloprotease, Proteinases, Proteases, PD166793, Matrix, Metalloprotease, Matrix, Metalloprotease, Tocris Bioscience
