P0047

PD166793 hydrate

≥98% (HPLC)

• Synonym(s): (S)-2-(4′-Bromo-biphenyl-4-sulfonylamino)-3-methyl-butyric acid hydrate
• Empirical Formula (Hill Notation): C₁₇H₁₈BrNO₄S · xH₂O
• CAS Number: 1228078-64-5
• Molecular Weight: 412.30 (anhydrous basis)
• MDL number: MFCD12912437
• UNSPSC Code: 12352200
• PubChem Substance ID: 329819997
• NACRES: NA.77

Properties

• assay: ≥98% (HPLC)
• form: solid
• storage temp.: 2-8°C
• SMILES string: O.CC(C)[C@H](NS(=O)(=O)c1ccc(cc1)-c2ccc(Br)cc2)C(O)=O
• InChI: 1S/C17H18BrNO4S.H2O/c1-11(2)16(17(20)21)19-24(22,23)15-9-5-13(6-10-15)12-3-7-14(18)8-4-12;/h3-11,16,19H,1-2H3,(H,20,21);1H2/t16-;/m0./s1
• InChI key: LUKRECOTGXWIDO-NTISSMGPSA-N

Description

Biochem/physiol Actions

PD166793 is a broad spectrum, but class-selective, MMP inhibitor (low nM at MMP-2 & 3 and low μM at MMP-1, 7 & 9). Adding PD166793 to the high-fat diet substantially reduced the rise in blood glucose. The improvement of glucose homeostasis in PD166793-treated ZDF rats was a result of the enhancement of β-cell function. It prevents β-cell dysfunction and diabetes in female ZDF rats on a high-fat diet. It has been shown to block left ventricular remodeling and dysfunction in a rat model of heart failure. Preservation of normoglycemia and normal glucose tolerance in compound PD166793-treated animals is accompanied by preservation of the high serum insulin levels that are a consequence of the insulin resistance present in these animals. It is not reversing insulin resistance these animals. The most striking effect of the compound is on pancreatic insulin content and β-cell volume.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable
• ppe: Eyeshields, Gloves, type N95 (US)