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EX00000246

Chemical Structure : EX00000246

CAS No.: 878292-27-4

EX00000246 (EX 00000246)

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

EX00000246 is a highly potent GPR5 (GPBAR1) agonist with EC50 of 2 nM in AlphaScreen cAMP assays.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

EX00000246 is a highly potent GPR5 (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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