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You are here:Home-Chemical Inhibitors & Agonists-GPCR-TGR5 (GPCR19, GPR131, GPBAR1)-EX00000246
EX00000246

Chemical Structure : EX00000246

CAS No.: 878292-27-4

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EX00000246 (EX 00000246)

Catalog No.: PC-20445Not For Human Use, Lab Use Only.

EX00000246 is a highly potent TGR5 (GPBAR1) agonist with EC50 of 2 nM in AlphaScreen cAMP assays.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    EX00000246 is a highly potent TGR5 (GPBAR1) agonist with EC50 of 2 nM in AlphaScreen cAMP assays.
    EX00000246 (500 nM) reduces cytokine production induced by various TLR ligands in human monocytes, also reduces CCL2, IL-12p70, and CXCL10, does not limit LPS induced IL-1β and IL-6 production.
    EX00000246 modulates a subset of LPS activated genes and blocks M1 differentiation in human monocytes.

    Physicochemical Properties

    M.Wt 393.42
    Formula C22H20FN3O3
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    7-fluoro-4-(2-(isoquinolin-5-yloxy)acetyl)-1,3,3-trimethyl-3,4-dihydroquinoxalin-2(1H)-one

    References

    1. Nuruddeen D Lewis, et al. PLoS One. 2014 Jun 26;9(6):e100883.

    2. PCT WO 2010/016552 A1.

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