| 名称 | Siponimod |
| 描述 | BAF312 (Siponimod (BAF-312)), a next-generation S1P receptor modulator, is specific for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, respectively. The specificity of BAF312 for S1P1 and S1P5 receptors exhibits >1000-fold over S1P2, S1P3 and S1P4 receptors. |
| 细胞实验 | Agonist-mediated internalization of S1P1 receptors in CHO cells analysed by flow cytometry Myc-tag hS1P1 cells are incubated for 1 h with agonist at 37°C in standard culture medium followed by a PBS wash. An aliquot is kept on ice for 3 h, while another aliquot is left for 3 (or 12) h in culture medium (no agonist) at 37°C. The cells are then incubated either with 4 μg/mL 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 of Alexa488-labelled goat anti-mouse secondary conjugates. The cells are subjected to flow cytometry measurements using 10000 viable cells per sample.(Only for Reference) |
| 激酶实验 | GTPγ[35S] binding assay: The cells are homogenized and centrifuged at 26900 × g for 30 min at 4°C. Membranes are re-suspended in 20 mM HEPES (pH 7.4), 100 mM NaCl, 10 mM MgCl2, 1 mM EDTA and 0.1% fat-free BSA at 2–3 mg protein/mL. GTPγ[35S] binding assay is performed with the membranes (75 mg protein /mL in 50 mM HEPES, 100 mM NaCl, 10 mM MgCl2, 20 μg/mL saponin and 0.1% fat-free BSA (pH 7.4), 5 mg/mL with wheat-germ agglutinin-coated scintillation proximity assay-bead, and 10 μM GDP for 10–15 min. The GTPγ[35S]-binding reaction is started by the addition of 200 pM GTPγ[35S]. After 120 min at room temperature, the plates are centrifuged for 10 min at 300 × g and counted. |
| 体外活性 | 在小鼠体内BAF312的预防或治疗剂量为0.3 mg/kg.在大鼠中,BAF312通过内化S1P1受体,从而有效抑制大鼠脑脊髓炎. |
| 体内活性 | BAF312 是有效的选择性S1P受体激动剂。它对S1P1和S1P5受体的EC50 分别为 0.39 nM 和 0.98 nM,并且对S1P1和S1P5受体的效力高于S1P2,S1P3 和 S1P4受体1000多倍。 |
| 存储条件 | keep away from moisture,keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : 41 mg/mL (79.37 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (1.94 mM), Sonication is recommended.
DMSO : 29.71 mg/mL (57.51 mM), Sonication is recommended.
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| 关键字 | Siponimod | S1PReceptor | S1P5 | S1P4 | S1P3 | S1P2 | S1P1 agonist | S1P1 | S1P Receptor | S1P receptor | progressive | neurodegeneration | multiple sclerosis | Lysophospholipid Receptor | lymphocytes | LPLReceptor | LPL Receptor | LPL | Inhibitor | inhibit | inflammation | BAF312 | BAF 312 |
| 相关产品 | Sphingosine-1-phosphate | S1PR1 modulator 1 | Ozanimod | LX-2931 | Ceranib-2 | SLP9101555 | Ki16198 | MP-A08 | Fingolimod hydrochloride | CYM50374 | CYM50260 | ASP-4058 |
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