An antagonist of EP4
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ER-819762

Item No. 10531

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(10S)-1′-[(3,5-dimethylphenyl)methyl]-2-ethyl-5,10-dihydro-7,9-dimethoxy-10-methyl-spiro[1H-imidazo[1,5-b][2]benzazepine-1,4′-piperidin]-3(2H)-one
CAS Number
1155773-15-1
Molecular Formula
C30H39N3O3
Formula Weight
489.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 50 mg/ml
SMILES
O=C1N(CC)C2(CCN(CC3=CC(C)=CC(C)=C3)CC2)C4=C[C@H](C)C5=C(C=C(OC)C=C5OC)CN41
InChi Code
InChI=1S/C30H39N3O3/c1-7-33-29(34)32-19-24-16-25(35-5)17-26(36-6)28(24)22(4)15-27(32)30(33)8-10-31(11-9-30)18-23-13-20(2)12-21(3)14-23/h12-17,22H,7-11,18-19H2,1-6H3/t22-/m0/s1
InChi Key
ANKFBAJRCGOKJJ-QFIPXVFZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

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    Product Description

    ER-819762 is an antagonist of the prostaglandin E2 (PGE2; Item No. 14010) receptor subtype EP4 (IC50 = 70 nM).1 It is selective for EP4 over EP1, EP2, and EP3 in a cAMP reporter assay at 10 µM. ER-819762 reduces differentiation of mouse helper T cells when used at concentrations ranging from 0.1 to 10 nM and decreases IL-23 secretion by mouse dendritic cells from 0.04 to 5 nM. It also reduces the levels of Marek's disease virus (MDV) in chicken embryonic fibroblasts (CEFs) when used at a concentration of 1 µM.2 Oral administration of ER-819762 (30 and 100 mg/kg) prevents and reverses paw swelling, edema, and inflammation in a mouse model of rheumatoid arthritis induced by glucose-6-phosphate isomerase (GPI).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chen, Q., Muramoto, K., Masaaki, N., et al. A novel antagonist of the prostaglandin E2 EP4 receptor inhibits Th1 differentiation and Th17 expansion and is orally active in arthritis models. Br. J. Pharmacol. 160(2), 292-310 (2010).

    2. Boodhoo, N., Kamble, N., Kaufer, B.B., et al. Replication of Marek’s disease virus is dependent on synthesis of de novo fatty acid and prostaglandin E2. J. Virol. 93(13), e00352-00319 (2109).