E7046 (ER-886406)

Catalog No.S6649 Batch:S664901

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Technical Data

Formula

C22H18F5N3O4
Molecular Weight 483.39 CAS No. 1369489-71-3
Solubility (25°C)* In vitro DMSO 100 mg/mL (206.87 mM)
 
 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description E7046 (ER-886406, Palupiprant, AN0025) is a selective inhibitor of the prostaglandin E2 (PGE2) receptor EP4 with IC50 of 13.5 nM and Ki of 23.14 nM.
Targets
EP4 [1]
(Cell-free assay)		 EP4 [1]
(Cell-free assay)
13.5nM 23.14 nM(Ki)
In vitro

E7046 has specific and potent inhibitory activity on PGE2-mediated pro-tumor myeloid cell differentiation and activation.[1]
In vivo

E7046 treatment reduces the growth or even rejected established tumors in vivo in a manner dependent on both myeloid and CD8+ T cells.[1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Monocytes

  • Concentrations

    10,100,300,1000,or 3000 nM

  • Incubation Time

    7d

  • Method

    Monocytes are placed in culture with recombinant human GM-CSF (20 ng/mL) + human IL-4 (500 U/mL) ± PGE2 (10 nM) ± E7046 (10,100,300,1000,or 3000 nM) for 7 d.
Animal Study:

[1]
  • Animal Models

    C57BL/6 mice

  • Dosages

    100 mg/kg or 150 mg/kg

  • Administration

    oral

Selleck's E7046 (ER-886406) has been cited by 1 publication

Macrophages evoke autophagy of hepatic stellate cells to promote liver fibrosis in NAFLD mice via the PGE2/EP4 pathway [ Cell Mol Life Sci, 2022, 79(6):303] PubMed: 35588334

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.