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Ceralifimod

(Synonyms: ONO-4641) 目录号 : GC18348

An agonist of S1P1 and S1P5 receptors

Ceralifimod Chemical Structure

Cas No.:891859-12-4

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1mg
¥444.00
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5mg
¥1,301.00
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10mg
¥1,951.00
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25mg
¥4,298.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Animal experiment:

Rats[1]Female Lewis rats are immunized by subcutaneous administration of the inducer at a volume of 0.1 mL into the footpad. Ceralifimod (ONO-4641: 0.01, 0.03 and 0.1 mg/kg), prednisolone (3 mg/kg) or 0.5% MC is administered orally once daily from immunization days 4-21. More specifically, the severity of paralysis is graded on a scoring scale to determine the clinical score. Mouse[1]NOD mice are immunized into the left footpad with the inducer at a volume of 0.05 mL. A second PTX injection is administered 48 h later. Animals that achieve remission after the initial onset are selected and grouped, and Ceralifimod (ONO-4641: 0.01, 0.03 or 0.1 mg/kg) or 0.5% MC is administered orally to each group once daily for 8 weeks. Neurological symptoms are graded according to the degree of paralysis. A clinical score of 5 is assigned to dead animals until the end of observation[1].

References:

[1]. Komiya T, et al. Efficacy and immunomodulatory actions of ONO-4641, a novel selective agonist for sphingosine 1-phosphate receptors 1 and 5, in preclinical models of multiple sclerosis. Clin Exp Immunol. 2013 Jan;171(1):54-62.

产品描述

Ceralifimod (ONO-4641) is selective, high potent agonist for sphingosine 1-phosphate receptors 1 and 5, with EC50s of 27.3, 334 pM for human S1P receptor 1 and 5, respectively.

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[1].

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[1].

References:
[1]. Komiya T, et al. Efficacy and immunomodulatory actions of ONO-4641, a novel selective agonist for sphingosine 1-phosphate receptors 1 and 5, in preclinical models of multiple sclerosis. Clin Exp Immunol. 2013 Jan;171(1):54-62.

Chemical Properties

Cas No. 891859-12-4 SDF
别名 ONO-4641
化学名 1-[[3,4-dihydro-6-[(2-methoxy-4-propylphenyl)methoxy]-1-methyl-2-naphthalenyl]methyl]-3-azetidinecarboxylic acid
Canonical SMILES CCCC1=CC=C(COC2=CC(CCC(CN3CC(C(O)=O)C3)=C4C)=C4C=C2)C(OC)=C1
分子式 C27H33NO4 分子量 435.6
溶解度 DMF: 5 mg/ml,DMSO: 5 mg/ml,DMSO:PBS (pH 7.2)(1:9): 0.1 mg/ml,Ethanol: slightly soluble 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.2957 mL 11.4784 mL 22.9568 mL
5 mM 0.4591 mL 2.2957 mL 4.5914 mL
10 mM 0.2296 mL 1.1478 mL 2.2957 mL
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