Cenerimod (ACT-334441) is a potentially first-in-class (first-in-class), potent, highly selective, orally active sphingosine 1-phosphate 1 (S1P1) receptor agonist with an EC50 value of 2.7 nM for use in studies related to systemic lupus erythematosus (SLE).
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Wistar rats |
| Formulation | 100% DMSO |
| Dosages | 10 mg/kg |
| Administration | oral |
| Molecular Weight | 453.53 |
| Formula | C25H31N3O5 |
| CAS Number | 1262414-04-9 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
| Related S1P Receptor Products |
|---|
| VTX-002
VTX-002 is an orally active, selective S1P receptor 1 modulator for studies related to ulcerative colitis. |
| TRV045
TRV045 is an S1P receptor modulator that can be used in studies related to central nervous system disorders. |
| S1PR1 modulator 1
S1PR1 modulator 1 is a selective S1PR1 inhibitor, with a pIC50 of 7.6, with >40- and >80-fold selectivity, over the other S1PR isoforms S1PR2/3/4. |
| Ozanimod hydrochloride
Ozanimod (RPC-1063) hydrochloride, a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod hydrochloride has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod hydrochloride can be used for the research of relapsing multiple sclerosis (MS) . |
| Icanbelimod
Icanbelimod (S1p receptor agonist 1) is a potent and orally active S1P1 receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). Icanbelimod has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). |
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