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Ceralifimod

Cat. No. M30823
Ceralifimod Structure
Synonym:

ONO-4641

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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 435.56
Formula C27H33NO4
CAS Number 891859-12-4
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Reshmi Roy, et al. CNS Drugs. Sphingosine 1-Phosphate Receptor Modulators for Multiple Sclerosis

[2] Haruto Kurata, et al. J Med Chem. Discovery of a 1-Methyl-3,4-dihydronaphthalene-Based Sphingosine-1-Phosphate (S1P) Receptor Agonist Ceralifimod (ONO-4641). A S1P1 and S1P5 Selective Agonist for the Treatment of Autoimmune Diseases

[3] Adnan M Subei, et al. CNS Drugs. Sphingosine 1-phosphate receptor modulators in multiple sclerosis

[4] Sonja Krösser, et al. J Clin Pharmacol. Effect of ceralifimod (ONO-4641) on lymphocytes and cardiac function: Randomized, double-blind, placebo-controlled trial with an open-label fingolimod arm

[5] Pedro J Gonzalez-Cabrera, et al. F1000Prime Rep. S1P signaling: new therapies and opportunities

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  Catalog
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