| Identification | Back Directory | [Name]
R243 | [CAS]
688352-84-3 | [Synonyms]
R243
6H-1,3-Dioxolo[4,5-g][1,3]benzoxazine, 7,8-dihydro-7-[2-(tricyclo[3.3.1.13,7]dec-1-yloxy)ethyl]-
7,8-Dihydro-7-[2-(tricyclo[3.3.1.1(3,7)]dec-1-yloxy)ethyl]-
6H-1,3-dioxolo[4,5-g][1,3]benzoxazine | [Molecular Formula]
C21H27NO4 | [MDL Number]
MFCD03829857 | [MOL File]
688352-84-3.mol | [Molecular Weight]
357.44 |
| Chemical Properties | Back Directory | [Boiling point ]
479.7±45.0 °C(Predicted) | [density ]
1.30±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 125 mg/mL (349.71 mM; Need ultrasonic) | [form ]
Solid | [pka]
4.81±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
R243 is a potent and selective CCR8 antagonist. R243 inhibits CCL1/CCR8 interaction and inhibits CCR8 signaling and chemotaxis. R243 has antinociceptive and anti-inflammatory effects[1][2]. | [in vivo]
R243 (0.1-1 mg/kg; intraperitoneal injection; once; male Swiss mice) treatment inhibits the analgesic effect evoked by CCL1 in a dose-dependent manner[2]. | Animal Model: | Male Swiss mice (7-9 weeks old) injected with CCL1[2] | | Dosage: | 0.1 mg/kg, 0.3mg/kg, 1 mg/kg | | Administration: |
Intraperitoneal injection; once | | Result: | The analgesic effect evoked by CCL1 (10 μg/kg; 1 h; s.c.) was dose-dependently inhibited.
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| [IC 50]
CCR8 | [References]
[1] Tomoyuki Oshio, et al. Chemokine Receptor CCR8 Is Required for Lipopolysaccharide-Triggered Cytokine Production in Mouse Peritoneal Macrophages. PLoS One. 2014 Apr 8;9(4):e94445. DOI:10.1371/journal.pone.0094445
[2] Mario García-Domínguez, et al. The Systemic Administration of the Chemokine CCL1 Evokes Thermal Analgesia in Mice Through the Activation of the Endocannabinoid System. Cell Mol Neurobiol. 2019 Nov;39(8):1115-1124. DOI:10.1007/s10571-019-00706-3 |
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