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Siponimod (BAF-312) 是有效,选择性的鞘氨醇-1-磷酸 (S1P)受体调节剂,对 S1P1 和 S1P5 受体具有特异性,EC50 分别为 0.39 nM 和 0.98 nM。 BAF312 对 S1P1 和 S1P5 受体的特异性比 S1P2、S1P3 和 S1P4 受体高 1000 倍以上。
Siponimod (BAF-312) 是有效,选择性的鞘氨醇-1-磷酸 (S1P)受体调节剂,对 S1P1 和 S1P5 受体具有特异性,EC50 分别为 0.39 nM 和 0.98 nM。 BAF312 对 S1P1 和 S1P5 受体的特异性比 S1P2、S1P3 和 S1P4 受体高 1000 倍以上。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 259 | 现货 | |
2 mg | ¥ 366 | 现货 | |
5 mg | ¥ 547 | 现货 | |
10 mg | ¥ 822 | 现货 | |
25 mg | ¥ 1,460 | 现货 | |
50 mg | ¥ 2,370 | 现货 | |
100 mg | ¥ 3,290 | 现货 | |
500 mg | ¥ 7,230 | 现货 |
产品描述 | 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. |
靶点活性 | S1P5 receptor:0.98 nM(EC50), S1P1 receptor:0.39 nM(EC50) |
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。 |
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. |
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) |
别名 | 辛波莫德, BAF-312 |
分子量 | 516.59 |
分子式 | C29H35F3N2O3 |
CAS No. | 1230487-00-9 |
Smiles | CCc1cc(ccc1CN1CC(C1)C(O)=O)C(C)=NOCc1ccc(C2CCCCC2)c(c1)C(F)(F)F |
密度 | 1.24 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: 41 mg/mL (79.4 mM) DMSO: 5.17 mg/mL (10 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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