| Identification | Back Directory | [Name]
S1p receptor agonist 1 | [CAS]
1514888-56-2 | [Synonyms]
CS-2465
YUN88562
icanbelimod
S1P-agonist-1
S1p receptor agonist 1
1-(2-fluoro-4-(5-(4-isobutylphenyl)-1,2,4-oxadiazol-3-yl)benzyl)azetidine-3-carboxylic acid
1-[[2-fluoro-4-[5-[4-(2-methylpropyl)phenyl]-1,2,4-oxadiazol-3-yl]phenyl]methyl]azetidine-3-carboxylic acid
3-Azetidinecarboxylic acid, 1-[[2-fluoro-4-[5-[4-(2-methylpropyl)phenyl]-1,2,4-oxadiazol-3-yl]phenyl]methyl]-
S1p receptor agonist 1,arthritis,Lysophospholipid Receptor,autoimmune,EAE,S-1p receptor agonist 1,sclerosis,encephalitis,Multiple,inhibit,Inhibitor,LPL Receptor | [Molecular Formula]
C23H24FN3O3 | [MOL File]
1514888-56-2.mol | [Molecular Weight]
409.45 |
| Chemical Properties | Back Directory | [Boiling point ]
566.3±60.0 °C(Predicted) | [density ]
1.268±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 6.8 mg/mL (16.61 mM) | [form ]
Solid | [pka]
2?+-.0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Icanbelimod (S1p receptor agonist 1) is a potent and orally active S1P receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). Icanbelimod has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). Icanbelimod is extracted from patent WO2015039587A1, Compound 2. | [in vivo]
Icanbelimod (oral administration; 0.01 mg/kg-1 mg/kg) at all dose is active, and only a dose of 0.01 mg/kg is required to observe a decrease in the number of peripheral blood lymphocytes by more than 50% and a decrease in the 1 mg/kg dose. Besides, this compound is lymphocyte-specific, which dose not significantly alter the number of peripheral monocytes and other white blood cells in SD rats[1].Icanbelimod (oral administration; 3 mg/kg; 12 days) is has been proved to block lymphocyte efflux. In the development of type II collagen-induced arthritis in rat model, compound 2 is effective in inhibiting the development of joint swelling in arthritis and joint structure destruction[1].Icanbelimod (oral administration; 0.3-1mg/kg; 30 days; once daily) inhibits the development of experimental autoimmune encephalitis (EAE) as a dose-dependent manner in mice model[1]. | Animal Model: | Lewis rats[1] | | Dosage: | 3 mg/kg | | Administration: | Oral administration | | Result: | Decreased the severity score of arthritis in the four-legged rats. |
| Animal Model: | Female C57BL/6 mice[1] | | Dosage: | 0.03, 0.1, and 1 mg/kg | | Administration: | Oral administration | | Result: | Decreased the severity score of EAE in MOG 35-55?induced mice. |
| [storage]
Store at -20°C | [References]
[1] Zhenwei, et al. Immune adjustment compound, use thereof and pharmaceutical composition comprising same. Patent WO2015039587A1 |
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| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
|