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251303-04-5

251303-04-5 Structure

251303-04-5 Structure
IdentificationBack Directory
[Name]

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

251303-04-5
[Synonyms]

PTP 112
Ertiprotafib
Benzenepropanoic acid, a-[4-(9-bromo-2,3-dimethylnaphtho[2,3-b]thien-4-yl)-2,6-dimethylphenoxy]-,(aR)-
Benzenepropanoic acid, α-[4-(9-bromo-2,3-dimethylnaphtho[2,3-b]thien-4-yl)-2,6-dimethylphenoxy]-, (αR)-
[Molecular Formula]

C31H27BrO3S
[MDL Number]

MFCD30532551
[MOL File]

251303-04-5.mol
[Molecular Weight]

559.51
Chemical PropertiesBack Directory
[Boiling point ]

690.7±55.0 °C(Predicted)
[density ]

1.376±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
[form ]

Solid
[pka]

3.21±0.10(Predicted)
[color ]

Light yellow to yellow
Hazard InformationBack Directory
[Uses]

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

As seen with treatment of ob/ob mice, both Ertiprotafib and compound 3 seem to significantly improve glucose metabolism in rats. At 25 mg/kg/day, these compounds decrease both fasting blood glucose and insulin levels compared with vehicle treated rats. Furthermore, both Ertiprotafib and compound 3 increase glucose disposal after an oral challenge. It is noteworthy that lipid levels are also reduced in treated animals. Both triglyceride and free fatty acid levels are substantially reduced in rats treated with 25 mg/kg/day of either compound. To summarize, both Ertiprotafib and compound 3 seem to be robust agents in improving glucose utilization in fa/fa rats while also decreasing lipid levels in these animals. Decreased lipid levels may be unexpected for a pure PTP1b inhibitor. It is more telling, as mentioned above, that rats treated with suprapharmacologic doses of Ertiprotafib show signs of PPAR family activation[2].

[IC 50]

PTP1B: 1.6 μM (IC50); IKK-β: 400 nM (IC50); PPARα: ~1 μM (EC50); PPARβ: ~1 μM (EC50)
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