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Ertiprotafib

Catalog No. T15243 CAS 251303-04-5

Synonyms: PTP 112

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).

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Ertiprotafib, CAS 251303-04-5

Pack Size	Availability	Price/USD
5 mg	8-10 weeks	$ 970.00
50 mg	8-10 weeks	$ 1,980.00
100 mg	8-10 weeks	$ 2,500.00

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

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( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Shrestha S, et al. PTP1B inhibitor Ertiprotafib is also a potent inhibitor of IkappaB kinase beta (IKK-beta). Bioorg Med Chem Lett. 2007 May 15;17(10):2728-30. Epub 2007 Mar 3. 2. Erbe DV, et al. Ertiprotafib improves glycemic control and lowers lipids via multiple mechanisms. Mol Pharmacol. 2005 Jan;67(1):69-77.

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Keywords

Ertiprotafib 251303-04-5 DNA Damage/DNA Repair Metabolism Phosphatase PPAR PTP 112 Inhibitor inhibitor inhibit

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