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产品价格:电议      采购度:1672      原产地:美洲
发布时间:2021/8/3 19:39:29 所属地区:上海 上海市
简要描述:
Ceralifimod (ONO-4641) 是 1-磷酸鞘氨醇受体 1 和 5 (S1P1 and S1P5) 的强效选择性激动剂,其对人 S1P1 和 S1P5 的 EC50 值分别为 ,334 pM。
标签:ONO-4641
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CAS No. : 891859-12-4
MCE 站:Ceralifimod
产品活性:Ceralifimod (ONO-4641) 是 1-磷酸鞘氨醇受体 1 和 5 (S1P1 and S1P5) 的强效选择性激动剂,其对人 S1P1 和 S1P5 的 EC50 值分别为 27.3,334 pM。
研究领域:GPCR/G Protein
作用靶点:LPL Receptor
In Vitro: Ceralifimod (ONO-4641) has an agonistic action for S1P1 and S1P5, and there is no difference between human and rat in the agonistic action of Ceralifimod (ONO-4641) for S1P1. Ceralifimod (ONO-4641) also induces S1P1 down-regulation in a concentration-dependent manner and by approximately 90% at concentration of 25 nM.
In Vivo: The clinical scores of the Ceralifimod (ONO-4641) 0.03 and 0.1 mg/kg groups remain lower than that in the control group. The maximum clinical scores decrease dose-dependently in the Ceralifimod (ONO-4641) groups and those in the Ceralifimod (ONO-4641) 0.03 and 0.1 mg/kg groups are significantly lower than that in the control group. Specifically, paralysis is inhibited completely in seven of eight animals in the Ceralifimod (ONO-4641) 0.1 mg/kg group.
In normal NOD mice, the number of peripheral blood lymphocytes is decreased by approximately 20, 60 and 80% at 24 h after a single oral dose of 0.01, 0.03 and 0.1 mg/kg of Ceralifimod (ONO-4641), respectively. In the control group of the NOD mouse model of relapsing-remitting EAE, the relapse rate is 90.0%, and two of the nine animals die. The cumulative clinical score in the control group is 65.4±18.50. In contrast, none of animals in the Ceralifimod (ONO-4641) 0.1 mg/kg group have a relapse; that is, Ceralifimod completely prevents relapse at a dose of 0.1 mg/kg. In the Ceralifimod (ONO-4641) groups, two of the nine animals in the 0.01 mg/kg die.
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更新时间:2024/1/2 10:17:57
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