Benzenepropanoicacid,a-[4-(9-bromo-2,3-dimethylnaphtho[2,3-b]thien-4-yl)-2,6-dimethylphenoxy]-,(aR)-

Ertiprotafib belongs to a novel class of insulin sensitizers developed for treatment of type 2 diabetes. In insulin-resistant rodent models, ertiprotafib and a close analog lowered both fasting blood glucose and insulin levels and improved glycemic excursion during an oral glucose tolerance test.|Ertiprotafib is an inhibitor of the protein tyrosine phosphatase 1B (PTP1B) and dual peroxisome proliferator-activated receptor (PPAR) alpha and gamma agonist with hypoglycemic and anti-lipidemic activity. Ertiprotafib inhibits PTP1B preventing the dephosphorylation of the insulin receptor, which improves insulin sensitivity and decreases blood glucose levels. In addition, this agent is able to stimulate both PPAR alpha and gamma thereby further improving glucose homeostasis and reducing triglyceride (TG) and free fatty acid levels. Ertiprotafib was also shown to be a potent inhibitor of IkappaB kinase beta (IKKbeta), which cotributes to its anti-inflammatory properties.

Treatment of non-insulin dependent diabetes (protein tyrosine phosphatase 1B inhibitor).

Molecular Weight:559.5
XLogP3:9.2
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:6
Exact Mass:558.08643
Monoisotopic Mass:558.08643
Topological Polar Surface Area:74.8
Heavy Atom Count:36
Complexity:744
Defined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes