Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Ertiprotafib is a PTP1B, IkB kinase β (IKK-β), and a dual <a href="/target/PPAR" style="display: inline; color: #c13a36">PPAR</a>α and <a href="/target/PPAR" style="display: inline; color: #c13a36">PPAR</a>β agonist inhibitor ( IC50s: 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for <a href="/target/PPAR" style="display: inline; color: #c13a36">PPAR</a>α/<a href="/target/PPAR" style="display: inline; color: #c13a36">PPAR</a>β).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | 8-10 weeks | $ 970.00 | |
50 mg | 8-10 weeks | $ 1,980.00 | |
100 mg | 8-10 weeks | $ 2,500.00 |
Description | Ertiprotafib is a PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist inhibitor ( IC50s: 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ). |
Targets&IC50 | PTP1B:1.6 μM, PPARβ:~1 μM (EC50), PPARα:~1 μM (EC50), IKK-β:400 nM |
In vitro | Ertiprotafib is a potent IKK-β inhibitor (IC50: 400 nM), which is much lower than that required for the half-maximal inhibition of the p-nitrophenyl phosphatase activity of PTP1B. Ertiprotafib is at least a dual PPARα and PPARβ agonist with EC50 values for transactivation of 1 μM. The reported IC50 value of Ertiprotafib against PTP1B ranges from 1.6 to 29 μM depending on the assay conditions [2]. Such activities readily explain the observations with suprapharmacologic doses of these [1]. |
In vivo | As seen with the treatment of ob/ob mice, both Ertiprotafib and compound 3 seem to obviously improve glucose metabolism in rats. Both Ertiprotafib and compound 3 increase in glucose disposal after an oral challenge. It is noteworthy that lipid levels are also reduced in treated animals. At 25 mg/kg/day, these compounds reduce both fasting blood glucose and insulin levels compared with vehicle-treated rats. Both triglyceride and free fatty acid levels are substantially reduced in rats treated with 25 mg/kg/day of either compound. Decreased lipid levels may be unexpected for a pure PTP1b inhibitor. As mentioned above, that rats treated with suprapharmacologic doses of Ertiprotafib display signs of PPAR family activation [2]. |
Synonyms | PTP 112 |
Molecular Weight | 559.51 |
Formula | C31H27BrO3S |
CAS No. | 251303-04-5 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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Ertiprotafib 251303-04-5 DNA Damage/DNA Repair Metabolism Phosphatase PPAR PTP 112 Inhibitor inhibitor inhibit