An EP2 receptor antagonist
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TG11-77 (hydrochloride)

Item No. 30188

Technical Information
Formal Name
2-((4,6-dimethylpyridin-2-yl)amino)-N-(2-(2-methyl-1H-indol-3-yl)ethyl)pyrimidine-5-carboxamide, monohydrochloride
CAS Number
2550393-38-7
Molecular Formula
C23H24N6O • HCl
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml
λmax
225, 261, 324 nm
SMILES
O=C(C1=CN=C(NC2=NC(C)=CC(C)=C2)N=C1)NCCC3=C(C)NC4=C3C=CC=C4.Cl
InChi Code
InChI=1S/C23H24N6O.ClH/c1-14-10-15(2)27-21(11-14)29-23-25-12-17(13-26-23)22(30)24-9-8-18-16(3)28-20-7-5-4-6-19(18)20;/h4-7,10-13,28H,8-9H2,1-3H3,(H,24,30)(H,25,26,27,29);1H
InChi Key
KNHQNXHZXZHWSS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    TG11-77 is a brain-permeable antagonist of the prostaglandin E2 (PGE2) receptor subtype EP2 (KB = 9.7 nM).1 It is selective for EP2 over DP1, EP4, and IP receptors (KBs = 7,320, 5,300, and >10,000 nM, respectively). TG11-77 (0.3 and 1 μM) inhibits the expression of genes encoding COX-2, IL-1β, and IL-6 induced by LPS and the EP2 receptor agonist ONO-AE1-259-01 in mouse BV-2 microglia expressing human EP2 receptors.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Amaradhi, R., Banik, A., Mohammed, S., et alPotent, selective, water soluble, brain-permeable EP2 receptor antagonist for use in central nervous system disease models. J. Med. Chem. 63(3), 1032-1050 (2020).