Ceralifimod

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

下一代 S1P 受体激动剂，对 S1P1 和 S1P5 具有选择性，EC50 分别为 0.0273 nM 和 0.334 nM。

A next-generation S1P receptor agonist selective for S1P1 and S1P5 with EC50 of 0.0273 nM and 0.334 nM; decreases peripheral blood lymphocyte counts in rats by inhibiting lymphocyte egress from secondary lymphoid tissues; inhibits lymphocyte infiltration into the spinal cord in a dose-dependent manner at doses of 0.03 and 0.1 mg/kg in a rat EAE model.Multiple Sclerosis.

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.

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.

ONO-4641 | ONO4641 | MSC-2430913A

GPCR/G Protein

Lysophospholipid Receptor

Lysophospholipid Receptor

Inflammation/Immunology

Multiple Sclerosis

891859-12-4

435.56

C27H33NO4

>98% (HPLC)

In Vitro:?DMSO : 2.86 mg/mL (6.57 mM)

CCCC1=CC=C(COC2=CC(CCC(CN3CC(C(O)=O)C3)=C4C)=C4C=C2)C(OC)=C1

1-[[6-[(2-Methoxy-4-propylbenzyl)oxy]-1-methyl-3,4-dihydro-2-naphthalenyl]methyl]azetidine-3-carboxylic acid

(-20℃)

With Ice Pack

≥ 2 years