2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. ER-819762

ER-819762 is an orally active, highly selective prostaglandin E2 (PGE2) EP4 receptor antagonist with an EC50 of 70 nM against human EP4 receptor. ER-819762 can be used for rheumatoid arthritis research.

For research use only. We do not sell to patients.

ER-819762 Chemical Structure

ER-819762 Chemical Structure

CAS No. : 1155773-15-1

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ER-819762 Related Antibodies

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Description

ER-819762 is an orally active, highly selective prostaglandin E2 (PGE2) EP4 receptor antagonist with an EC50 of 70 nM against human EP4 receptor. ER-819762 can be used for rheumatoid arthritis research[1].

IC50 & Target

EP4

70 nM (IC50)

In Vitro

ER-819762 suppresses human EP4 receptor-mediated cell signalling as measured in a cAMP-dependent reporter assay (IC50 value of 59 ± 6 nM)[1].
ER-819762 (0-10 μM, 3 days) selectively suppresses PGE2-induced Th1 differentiation[1].
ER-819762 (0-5 μM, 24 h) suppresses IL-23 secretion in human monocyte-derived dendritic cells[1].
ER-819762 (0.1 and 1 μM, 3 days) suppresses IL-17 production and inhibits IL-23-induced Th17 expansion in activated CD4+ T cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ER-819762 Related Antibodies
In Vivo

ER-819762 (0-100 mg/kg; p.o.; daily) suppresses inflammatory arthritis in mice[1].
ER-819762 (0-100 mg/kg; p.o.; once) suppresses CFA (Freund’s adjuvant)-induced hyperalgesia in rat[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male DBA/1 mice, collagen-induced arthritis (CIA) model and GPI (glucose-6-phosphate isomerase)-induced arthritis model[1]
Dosage: 10, 30 and 100 mg/kg
Administration: Oral; daily; in CIA model: from day 20 after primary immunization but before disease onset (prophylactic evaluation) or after the disease induction (therapeutic evaluation), in GPI-induced arthritis model: from day 6 after primary immunization but before disease onset (prophylactic evaluation) or after the disease induction (therapeutic evaluation).
Result: Dose-dependently suppressed the clinical signs of arthritis and delayed disease onset, significantly suppressed disease progression when administered subsequent to the onset of disease and retarded bone erosion in the CIA model. In the GPI-induced arthritis model, significantly reduced arthritis severity and delayed disease onset when administered prior to the onset of disease and also significantly suppressed disease progression when administered after the establishment of arthritis.
Animal Model: Male F344 rats, CFA-induced hyperalgesia model[1]
Dosage: 10, 30 and 100 mg/kg
Administration: Oral, once
Result: Significantly suppressed lame walk reaction.
Molecular Weight

489.65

Formula

C30H39N3O3
CAS No.
SMILES

CCN1C2(CCN(CC2)CC3=CC(C)=CC(C)=C3)C(N(CC4=CC(OC)=C5)C1=O)=C[C@H](C)C4=C5OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ER-819762 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ER-8197621155773-15-1ER819762ER 819762Prostaglandin Receptorrheumatoid arthritischronic inflammatory painhyperalgesiaInhibitorinhibitorinhibit

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