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编 号：F048848
分子式：C30H39N3O3
分子量：489.65
分子式：C30H39N3O3
分子量：489.65
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CAS No: 1155773-15-1
产品详情
生物活性：
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.
体内研究：
ER-819762 (0-100 mg/kg; p.o.; daily) suppresses inflammatory arthritis in mice.ER-819762 (0-100 mg/kg; p.o.; once) suppresses CFA (Freund’s adjuvant)-induced hyperalgesia in rat.Animal Model:Male DBA/1 mice, collagen-induced arthritis (CIA) model and GPI (glucose-6-phosphate isomerase)-induced arthritis model
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
Dosage:10, 30 and 100 mg/kg
Administration:Oral, once
Result:Significantly suppressed lame walk reaction.
体外研究：
ER-819762 suppresses human EP4 receptor-mediated cell signalling as measured in a cAMP-dependent reporter assay (IC50 value of 59 ± 6 nM).ER-819762 (0-10 μM, 3 days) selectively suppresses PGE2-induced Th1 differentiation.ER-819762 (0-5 μM, 24 h) suppresses IL-23 secretion in human monocyte-derived dendritic cells.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.
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.
体内研究：
ER-819762 (0-100 mg/kg; p.o.; daily) suppresses inflammatory arthritis in mice.ER-819762 (0-100 mg/kg; p.o.; once) suppresses CFA (Freund’s adjuvant)-induced hyperalgesia in rat.Animal Model:Male DBA/1 mice, collagen-induced arthritis (CIA) model and GPI (glucose-6-phosphate isomerase)-induced arthritis model
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
Dosage:10, 30 and 100 mg/kg
Administration:Oral, once
Result:Significantly suppressed lame walk reaction.
体外研究：
ER-819762 suppresses human EP4 receptor-mediated cell signalling as measured in a cAMP-dependent reporter assay (IC50 value of 59 ± 6 nM).ER-819762 (0-10 μM, 3 days) selectively suppresses PGE2-induced Th1 differentiation.ER-819762 (0-5 μM, 24 h) suppresses IL-23 secretion in human monocyte-derived dendritic cells.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.
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