辛波莫德 T6403

Product Introduction
Bioactivity


英文名: Siponimod

描述: 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。

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: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 41 mg/mL (79.4 mM)
DMSO : 5.17 mg/mL (10 mM)


关键字: inflammation | Lysophospholipid Receptor | S1P receptor | inhibit | neurodegeneration | Siponimod | S1P1 agonist | progressive | multiple sclerosis | lymphocytes | BAF312 | LPL Receptor | BAF 312 | Inhibitor

相关产品: VPC 23019 | CYM50308 | SphK1&2-IN-1 | MHP | Fingolimod | GLPG2938 | W140 HBr | SLP9101555 | Peretinoin | Sphingosine-1-phosphate

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Approved Drug Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | Highly Selective Inhibitor Library | EMA Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途