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

Ceralifimod  (Synonyms: ONO-4641)

Cat. No.: HY-12685
Handling Instructions

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.

For research use only. We do not sell to patients.

Ceralifimod Chemical Structure

Ceralifimod Chemical Structure

CAS No. : 891859-12-4

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Description

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].
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.
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
Molecular Weight

435.56

Formula

C27H33NO4
CAS No.
SMILES

O=C(C1CN(CC2=C(C)C3=C(C=C(OCC4=CC=C(CCC)C=C4OC)C=C3)CC2)C1)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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.
References
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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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Keywords:

Ceralifimod891859-12-4ONO-4641ONO4641ONO 4641LPL ReceptorLysophospholipid ReceptorInhibitorinhibitorinhibit

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