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BAF312 (Siponimod) is a next-generation S1P receptor modulator, selective for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors.
Brain. 2023 Mar 30;awad051.
Monitoring recovery after CNS demyelination, a novel tool to de-risk pro-remyelinating strategies
BAF312 purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | CHO cells |
| Preparation method | Agonist-mediated internalization of S1P1 receptors in CHO cells analysed by flow cytometry Myc-tag hS1P1 cells were incubated for 1 h with agonist at 37°C in standard culture medium followed by a PBS wash. An aliquot was kept on ice for 3 h, while another aliquot was left for 3 (or 12) h in culture medium (no agonist) at 37°C. The cells were then incubated either with 4 µg·mL−1 monoclonal mouse anti C-myc IgG1 antibody or with isotype control mouse IgG1 for 60 min at 4°C, followed by an incubation with 1 µg·mL−1 of Alexa488-labelled goat anti-mouse secondary conjugates. The cells were subjected to flow cytometry measurements using 10000 viable cells per sample. |
| Concentrations | 1 μM |
| Incubation time | 1h |
| Animal Experiment | |
|---|---|
| Animal models | EAE model in the DA rat |
| Formulation | 1% aqueous carboxy-methylcellulose |
| Dosages | 0.03, 0.3 and 3 mg/kg once daily |
| Administration | oral gavage |
| Molecular Weight | 516.6 |
| Formula | C29H35F3N2O3 |
| CAS Number | 1230487-00-9 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related S1P Receptor Products |
|---|
| FTY720 hydrochloride
Fingolimod (FTY720) HCl is a 1-phospho-neuraminol S1P receptor antagonist with an IC50 of 0.33 nM. , FTY720 can dephosphorylate AMPK by activating PP2A and reduce the expression level of phosphorylated eEF2K, ultimately leading to ADCD and iron death in human multiple myeloma cells. |
| SEW2871
SEW2871 is an orally active, potent, highly selective S1P1 (sphingosine-1-phosphate type 1 receptor) agonist, with an EC50 of 13.8 nM. SEW2871 activates ERK, Akt, and Rac signaling pathways and induces S1P1 internalization and recycling. |
| CYM-5442
CYM-5442 is a potent and selective S1P1 agonist with EC50 of 1.35 nM. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 can easily penetrate the central nervous system (CNS). |
| JTE 013
JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM. |
| KRP-203 hydrochloride
Mocravimod (KRP-203) hydrochloride is a potent, orally active sphingosine receptor S1P1 and S1P4 agonist with EC50s of 1 nM and 10 nM, respectively, and may be used in studies related to ulcerative colitis (UC). |
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