A potent and selective EP4 receptor antagonist
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BGC 20-1531 (hydrochloride)

Item No. 19742

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[4-(5-methoxy-2-pyridinyl)phenoxy]methyl]-5-methyl-N-[(2-methylphenyl)sulfonyl]-2-furancarboxamide, monohydrochloride
CAS Number
1962928-26-2
Synonyms
  • PGN 1531
Molecular Formula
C26H24N2O6S • HCl
Formula Weight
529.0
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/ml
λmax
202, 273 nm
SMILES
COC1=CN=C(C2=CC=C(OCC3=C(C)OC(C(NS(C4=CC=CC=C4C)(=O)=O)=O)=C3)C=C2)C=C1.Cl
InChi Code
InChI=1S/C26H24N2O6S.ClH/c1-17-6-4-5-7-25(17)35(30,31)28-26(29)24-14-20(18(2)34-24)16-33-21-10-8-19(9-11-21)23-13-12-22(32-3)15-27-23;/h4-15H,16H2,1-3H3,(H,28,29);1H
InChi Key
ZSHYZCXOFPPBMH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    Product Description

    BGC 20-1531 is a potent and selective antagonist of the prostaglandin E2 (PGE2; Item No. 14010) receptor subtype 4 (EP4) with Ki values of 11.7, >10,000, and >10,000 nM for EP4, EP2, and EP3, respectively.1 It is selective for EP4, exhibiting <50% inhibition at 47 ion channels, cell-surface transporters, enzymes, and nuclear receptors at a concentration of 10 μM. BGC 20-1531 antagonizes PGE2-induced cAMP accumulation in a dose-dependent manner in HEK293 EBNA cells that stably express human EP4 receptors. It also reverses PGE2-induced vasorelaxation (Kb = 15.85 nM) in human middle cerebral and middle meningeal arterial rings. BGC 20-1531 prevents PGE2-induced increases in carotid blood flow and decreases in carotid resistance with an ID50 value of 5 mg/kg in dogs.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Maubach, K.A., Davis, R.J., Clark, D.E., et al. BGC20-1531, a novel, potent and selective prostanoid EP4 receptor antagonist: A putative new treatment for migraine headache. Br. J. Pharmacol. 156(2), 316-327 (2009).