| Identification | Back Directory | [Name]
(10S)-1'-[(3,5-Dimethylphenyl)methyl]-2-ethyl-5,10-dihydro-7,9-dimethoxy-10-methylspiro[1H-imidazo[1,5-b][2]benzazepine-1,4'-piperidin]-3(2H)-one | [CAS]
1155773-15-1 | [Synonyms]
ER 819762
(10S)-1'-[(3,5-Dimethylphenyl)methyl]-2-ethyl-5,10-dihydro-7,9-dimethoxy-10-methylspiro[1H-imidazo[1,5-b][2]benzazepine-1,4'-piperidin]-3(2H)-one | [Molecular Formula]
C30H39N3O3 | [MDL Number]
MFCD31544488 | [MOL File]
1155773-15-1.mol | [Molecular Weight]
489.65 |
| Chemical Properties | Back Directory | [Boiling point ]
622.2±65.0 °C(Predicted) | [density ]
1.20±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
ethanol|2.45|5withgentlewarming|DMSO|0.98|2withgentlewarming| | [form ]
A solid | [pka]
9.31±0.40(Predicted) |
| Hazard Information | Back Directory | [Uses]
ER 819762 is a novel antagonist of the prostaglandin E2EP4 receptor, which also inhibits Th1 differentiation and Th17 expansion and is orally active in arthritis models. | [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. |
| [IC 50]
EP4: 70 nM (IC50) | [storage]
Store at -20°C |
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| Company Name: |
BOC Sciences
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| Tel: |
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| Website: |
https://www.bocsci.com |
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