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Purity: ≥98%
Ceralifimod (also known as ONO-4641) is a novel sphingosine-1-phosphate (S1P) receptor agonist selective for S1P1 and S1P5. While it has been demonstrated that treating autoimmune diseases like relapsing-remitting multiple sclerosis (RRMS) with modulation of the S1P1 receptor is effective, activation of the S1P3 receptor has also been linked to certain negative effects. The clinical candidate ceralifimod was found to be potent in a peripheral lymphocyte lowering (PLL) test in mice (ED50 = 0.029 mg/kg, 24 hours after oral dosing) and to have >30,000-fold selectivity for S1P1 over S1P3.
| Targets |
hS1P1 ( EC50 = 27.3 pM ); hS1P5 ( EC50 = 334 pM )
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| Enzyme Assay |
Ceralifimod (also known as ONO-4641) is a novel selective agonist of the sphingosine-1-phosphate (S1P) receptor that targets only S1P1 and S1P5.
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| Animal Protocol |
Rats: Inducer injections into the footpad at a volume of 0.1 mL are used to immunize female Lewis rats subcutaneously. Oral administration of ceralifimod (ONO-4641: 0.01, 0.03, and 0.1 mg/kg), prednisolone (3 mg/kg), or 0.5% MC is done once a day for immunization days 4 through 11. The clinical score is specifically determined by grading the degree of paralysis on a scoring scale.
Mouse: The inducer is injected into the left footpad of NOD mice at a volume of 0.05 mL. Forty-eight hours later, another PTX injection is given. Once every day for eight weeks, either 0.5% MC or Ceralifimod (ONO-4641: 0.01, 0.03, or 0.1 mg/kg) is given orally to each group of animals that achieve remission following the initial onset. The degree of paralysis determines how neurological symptoms are rated. Animals that are dead are given a clinical score of 5 until the end of the observation[1]. |
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| References |
| Molecular Formula |
C27H33NO4
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| Molecular Weight |
435.56
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| Exact Mass |
435.24
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| CAS # |
891859-12-4
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| Related CAS # |
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| Appearance |
White to off-white solid powder
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| SMILES |
CCCC1=CC(=C(C=C1)COC2=CC3=C(C=C2)C(=C(CC3)CN4CC(C4)C(=O)O)C)OC
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| InChi Key |
QDDQIPUKAXBMBX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H33NO4/c1-4-5-19-6-7-22(26(12-19)31-3)17-32-24-10-11-25-18(2)21(9-8-20(25)13-24)14-28-15-23(16-28)27(29)30/h6-7,10-13,23H,4-5,8-9,14-17H2,1-3H3,(H,29,30)
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| Chemical Name |
1-[[6-[(2-methoxy-4-propylphenyl)methoxy]-1-methyl-3,4-dihydronaphthalen-2-yl]methyl]azetidine-3-carboxylic acid
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2959 mL | 11.4795 mL | 22.9589 mL | |
| 5 mM | 0.4592 mL | 2.2959 mL | 4.5918 mL | |
| 10 mM | 0.2296 mL | 1.1479 mL | 2.2959 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01081782 | Completed | Drug: ONO-4641 Drug: ONO-4641 placebo |
Multiple Sclerosis | Ono Pharma USA Inc | March 2010 | Phase 2 |
| NCT01226745 | Terminated | Drug: ONO-4641 | Multiple Sclerosis | EMD Serono | October 2010 | Phase 2 |
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