ER-819762 是一种具有口服活性的、高选择性前列腺素 E2(PGE2)EP4受体拮抗剂，对人 EP4受体的EC50为 70 nM。 ER-819762 可用于类风湿关节炎的研究。
| 生物活性 | ER-819762 is an orally active, highly selective prostaglandin E2(PGE2)EP4receptorantagonist with anEC50of 70 nM against humanEP4receptor. ER-819762 can be used for rheumatoid arthritis research[1]. |
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体外研究
(In Vitro) | ER-819762 suppresses human EP4receptor-mediated cell signalling as measured in a cAMP-dependent reporter assay (IC50value 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].
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体内研究
(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].
| 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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