產(chǎn)品描述: | Esonarimod is an antirheumatic drug. |
靶點(diǎn): |
IL Receptor;ILReceptor |
體內(nèi)研究: |
After repeated oral administration of Esonarimod (14C-KE-298), the radioactivity decreases rapidly and no tendency towards accumulation is found |
細(xì)胞實(shí)驗(yàn): |
For in vitro experiment, Esonarimod (KE-298) is dissolved in ethanol and diluted with culture medium or distilled water.RAW264.7 cells are used in this study. For NO production, RAW264.7 cells [2×105/0.2 mL of RPMI-1640 supplemented by 10% heat inactivated fetal bovine serum (FBS), penicillin G (100 U/mL), and streptomycin (100 μg/mL)] are stimulated with 100 ng/mL of Escherichia coli 026:B6 lipopolysaccharide in the presence of Esonarimod (KE-298) (0, 10, 30, 100, 200, 300 μg/mL) in 96 well plates and incubated 24 h at 37°C in an atmosphere of 5% CO2 in air. After incubation, the supernatants are collected and assayed for nitrite (NO2-) instead of NO |
動(dòng)物實(shí)驗(yàn): |
Seven-week-old male Wistar rats is administered Esonarimod (5 mg/kg once daily) orally by gastric intubation |
參考文獻(xiàn): |
1.Inoue T, et al. KE-298 and its active metabolite KE-758 suppress nitric oxide production by murine macrophage cells and peritoneal cells from rats with adjuvant induced arthritis. J Rheumatol. 2001 Jun;28(6):1229-37. 2.Hasegawa M, et al. Formation of a disulfide protein conjugate of the SH-group-containing metabolite (M-I) ofesonarimod (KE-298) and its elimination in rats. J Pharm Pharmacol. 2002 Apr;54(4):493-8. |
溶解性: |
DMSO:10 mM |
保存條件: |
2-8℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
3.567 ml |
17.836 ml |
35.671 ml |
5 mM |
0.713 ml |
3.567 ml |
7.134 ml |
10 mM |
0.357 ml |
1.784 ml |
3.567 ml |
50 mM |
0.071 ml |
0.357 ml |
0.713 ml |
|
注意: |
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