[CAS NO. 891859-12-4] Ceralifimod
PRODUCTS SPECIFICATIONS [891859-12-4]
DESCRIPTION [891859-12-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 435.56 |
| Molecular Formula | C27H33NO4 |
| SMILES | O=C(C1CN(CC2=C(C)C3=C(C=C(OCC4=CC=C(CCC)C=C4OC)C=C3)CC2)C1)O |
Summary
Ceralifimod (ONO-4641) is selective, high potent agonist for sphingosine 1-phosphate receptors 1 and 5, with EC 50 s of 27.3, 334 pM for human S1P receptor 1 and 5, respectively.
IC50 & Target
EC50: 27.3 pM (hS1P 1 ), 334 pM (hS1P 5 ) [1] .
In Vitro
Ceralifimod (ONO-4641) has an agonistic action for S1P 1 and S1P 5 , and there is no difference between human and rat in the agonistic action of Ceralifimod (ONO-4641) for S1P 1 . Ceralifimod (ONO-4641) also induces S1P 1 down-regulation in a concentration-dependent manner and by approximately 90% at concentration of 25 nM [1] .
MedChemExpress (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]
.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01226745 | EMD Serono|Merck KGaA, Darmstadt, Germany|Ono Pharmaceutical Co. Ltd |
Multiple Sclerosis
|
October 2010 | Phase 2 |
| NCT01081782 | Ono Pharma USA Inc|Ono Pharmaceutical Co. Ltd |
Multiple Sclerosis
|
March 2010 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 2.86 mg/mL ( 6.57 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 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 |
| 10 mM | --- | --- | --- |