Ertiprotafib

SKU: orb1707329

Description

Ertiprotafib

Research Area

Metabolism Research, Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 251303-04-5
• MW: 559.51
• Purity: 98.38% (May vary between batches)
• Formula: C₃₁H₂₇BrO₃S
• SMILES: CC=1C2=C(C=3C(C(Br)=C2SC1C)=CC=CC3)C4=CC(C)=C(O[C@H](CC5=CC=CC=C5)C(O)=O)C(C)=C4
• Target: IκB/IKK,Phosphatase,PPAR
• Solubility: DMSO:80 mg/mL (142.98 mM);10% DMSO+90% Corn Oil:3.3 mg/mL (5.9 mM)

Bioactivity

• Target IC50:
  PTP1B:1.6 μM|PPARβ:~1 μM (EC50)|IKKβ:400 nM|PPARα:~1 μM (EC50)
• In Vivo:
  METHODS: Here, 11-week-old leptin-deficient male ob/ob mice were administered Ertiprotafib (25 mg/kg, daily, for 4 days), and changes in blood glucose indicators were observed. RESULTS: Mice treated with ertiprotafib had fasting blood glucose levels returned to the normal range, along with a significant decrease in insulin levels and a significant decrease in serum triglyceride levels.
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• In Vitro:
  METHODS: To measure the kinase activity of IKK-b, ertiprotafib was used in doses (0.001-1 μM) and a peptide substrate containing the IjB phosphorylation motif was used, and the phosphorylated peptide product was determined using an ELISA-type assay with time-resolved fluorescence (TRF) measurements. RESULTS: Ertiprotafib is a potent IKK-b inhibitor with an IC50 value of 400 ± 40 nM, which is well below the value required for half-maximal inhibition of PTP1B p-nitrophenyl phosphatase activity. The reported IC50 values ​​of ertiprotafib for PTP1B range from 1.6 to 29 μM, depending on the assay conditions.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

IκB, Ertiprotafib, IKK-β, IKKβ, IkB/IKK, IkB, IKK, PPARα, PPARβ, PTP 112, PTP112, PTP-112, PTP1B

Compound Identifiers

PubChem CID

157049