1. GPCR/G Protein
  2. LPL Receptor
  3. Ceralifimod

Ceralifimod  (Synonyms: ONO-4641)

目录号: HY-12685 纯度: 99.49%
COA 产品使用指南

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 S1P5EC50 值分别为 27.3,334 pM。

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Ceralifimod Chemical Structure

Ceralifimod Chemical Structure

CAS No. : 891859-12-4

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1 mg ¥300
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5 mg ¥870
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10 mg ¥1400
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25 mg ¥2800
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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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.

IC50 & Target

EC50: 27.3 pM (hS1P1), 334 pM (hS1P5)[1].

体外研究
(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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

435.56

Formula

C27H33NO4

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 2.86 mg/mL (6.57 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2959 mL 11.4795 mL 22.9590 mL
5 mM 0.4592 mL 2.2959 mL 4.5918 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

Ceralifimod 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2959 mL 11.4795 mL 22.9589 mL 57.3974 mL
5 mM 0.4592 mL 2.2959 mL 4.5918 mL 11.4795 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Ceralifimod
目录号:
HY-12685
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