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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 (Roche Applied Science, Mannheim, Germany) antibody or with isotype control mouse IgG1 (Pharmingen, BD Biosciences, Basel, Switzerland) for 60 min at 4°C, followed by an incubation with 1 µg·mL−1 of Alexa488-labelled goat anti-mouse secondary conjugates (Molecular Probes, Juro Supply, Luzern, Switzerland). 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 (C-4888, Sigma Chemical Co, St Louis, MO) |
| 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 |
|---|
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| 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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