| Identification | Back Directory | [Name]
Methanone, [(3S)-3-[[4-(1,1-dimethylethoxy)phenoxy]methyl]-6-fluoro-3,4-dihydro-2(1H)-isoquinolinyl]-1-naphthalenyl- | [CAS]
1801185-08-9 | [Synonyms]
SR12418
Methanone, [(3S)-3-[[4-(1,1-dimethylethoxy)phenoxy]methyl]-6-fluoro-3,4-dihydro-2(1H)-isoquinolinyl]-1-naphthalenyl- | [Molecular Formula]
C31H30FNO3 | [MOL File]
1801185-08-9.mol | [Molecular Weight]
483.57 |
| Chemical Properties | Back Directory | [Boiling point ]
645.1±55.0 °C(Predicted) | [density ]
1.191±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
-2.21±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
SR12418 is a REV-ERB-specific synthetic ligand with IC50s of 68 nM and 119 nM for REV-ERBα and REV-ERBβ, respectively. SR12418 can be used in experimental autoimmune encephalomyelitis (EAE) and colitis research[1][2]. | [in vivo]
SR12418 (intraperitoneal injection; 50 mg/kg; twice a day) suppresses the development and severity of experimental autoimmune encephalomyelitis[1].
SR12418 (intraperitoneal injection; 50 mg/kg; twice a day; begin at day 18 post-immunization) shows effects in intervention studies of relapsing-remitting experimental autoimmune encephalomyelitis[1]. | Animal Model: | C57BL/6 mice inducing experimental autoimmune encephalomyelitis (EAE)[1] | | Dosage: | 50 mg/kg | | Administration: | Intraperitoneal injection; 50 mg/kg; twice a day | | Result: | Diminished the incidence of disease with approximately 20% mice developing disease.
Showed no overt signs of toxicity. |
| Animal Model: | PLP139-151-induced relapsing-remitting EAE (R-EAE) in SJL/J mice[1] | | Dosage: | 50 mg/kg | | Administration: | Intraperitoneal injection; 50 mg/kg; twice a day; begin at day 18 post-immunization | | Result: | Resulted in a significant reduction in the relapse severity compared to the vehicle control.
Showed a significant decrease in the frequency and number of CD4+ and CD8+ effector cells (CD44hi). |
| [References]
[1] Mohammed Amir, et al. REV-ERBα Regulates TH17 Cell Development and Autoimmunity. Cell Rep. 2018 Dec 26;25(13):3733-3749.e8. DOI:10.1016/j.celrep.2018.11.101
[2] Shuai Wang, et al. Targeting REV-ERBα for therapeutic purposes: promises and challenges. Theranostics. 2020 Mar 4;10(9):4168-4182. DOI:10.7150/thno.43834 |
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