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.
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- CAS No.: 1155773-15-1
- Formule: C30H39N3O3
- Masse moléculaire:489.65
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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EP4 70 nM (IC50) |
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 (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.
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Animal Model:Male DBA/1 mice, collagen-induced arthritis (CIA) model and GPI (glucose-6-phosphate isomerase)-induced arthritis model[1]
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Dosage:10, 30 and 100 mg/kg
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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).
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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.
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Animal Model:Male F344 rats, CFA-induced hyperalgesia model[1]
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Dosage:10, 30 and 100 mg/kg
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Administration:Oral, once
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Result:Significantly suppressed lame walk reaction.
Chemical Information
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CAS No. 1155773-15-1
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Masse moléculaire 489.65
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Formule C30H39N3O3
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SMILES
CCN1C2(CCN(CC2)CC3=CC(C)=CC(C)=C3)C(N(CC4=CC(OC)=C5)C1=O)=C[C@H](C)C4=C5OC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ER-819762 Related Classifications
HY-116099 Related Classifications
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