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Cenerimod (ACT-334441) is a potent and orally available sphingosine 1-phosphate 1 receptor (S1P1) agonist extracted from patent WO 2016184939 A1 and WO 2011007324 A1, example 1, with an EC50 of 2.7 nM.
| Cell Experiment | |
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Wistar rats |
| Formulation | 100% DMSO |
| Dosages | 10 mg/kg |
| Administration | oral |
| 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.
| Molecular Weight | 453.53 |
| Formula | C25H31N3O5 |
| CAS Number | 1262414-04-9 |
| Purity | >98% |
| Solubility | 10 mM in DMSO |
| Storage | at -20°C |
Cenerimod, a novel selective S1P1 receptor modulator with unique signaling properties.
Piali L, et al. Pharmacol Res Perspect. 2017 Dec;5(6). PMID: 29226621.
Pharmacokinetics, Pharmacodynamics, Tolerability, and Food Effect of Cenerimod, a Selective S1P₁ Receptor Modulator in Healthy Subjects.
Juif PE, et al. Int J Mol Sci. 2017 Dec 6;18(12). PMID: 29211013.
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