Siponimod (BAF312)

製品コードS7179 バッチS717903

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C29H35F3N2O3
分子量 516.6 CAS No. 1230487-00-9
Solubility (25°C)* 体外 DMSO 100 mg/mL warmed with 50ºC water bath (193.57 mM)
Ethanol 25 mg/mL warmed with 50ºC water bath (48.39 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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. Phase 3.
in vitro BAF312 (Siponimod) is a potent and selective S1P receptor agonist, with EC50 of 0.39 nM and 0.98 nM for S1P1 and S1P5receptors, exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors. [1]BAF312 (1 h at 1 μM) promotes prominent internalization of S1P1 receptors by 91%.[2]
in vivo BAF312 effectively suppresses encephalomyelitis (EAE) in rats by internalizing S1P1 receptors, rendering them insensitive to the egress signal from lymph nodes. [1] BAF312 significantly reduces clinical scores when dosed prophylactically or therapeutically in mice at 0.3 mg/kg. [3]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 CHO
濃度 ~1 μM
反応時間 1 h
実験の流れ 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.
動物実験 動物モデル encephalomyelitis (EAE) model rat
投薬量 0.03, 0.3 and 3 mg/kg
投与方法 oral gavage

カスタマーフィードバック

Data from [Data independently produced by , , Leukemia, 2018, 32(1):214-223]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The Oncogenic Lipid Sphingosine-1-Phosphate Impedes the Phagocytosis of Tumor Cells by M1 Macrophages in Diffuse Large B Cell Lymphoma [ Cancers (Basel), 2024, 16(3)574] PubMed: 38339325
Siponimod ameliorates experimental autoimmune neuritis [ J Neuroinflammation, 2023, 20(1):35] PubMed: 36788526
Comprehensive metabolomics expands precision medicine for triple-negative breast cancer [ Cell Res, 2022, 10.1038/s41422-022-00614-0] PubMed: 35105939
Ponesimod inhibits astrocyte-mediated neuroinflammation and protects against cingulum demyelination via S1P1 -selective modulation [ FASEB J, 2022, 36(2):e22132] PubMed: 34986275
A Pipeline to Investigate the Structures and Signaling Pathways of Sphingosine 1-Phosphate Receptors [ J Vis Exp, 2022, (184).] PubMed: 35758708
The targetable nanoparticle BAF312@cRGD-CaP-NP represses tumor growth and angiogenesis by downregulating the S1PR1/P-STAT3/VEGFA axis in triple-negative breast cancer [ J Nanobiotechnology, 2021, 19(1):165] PubMed: 34059068
Nanoparticle BAF312@CaP-NP Overcomes Sphingosine-1-Phosphate Receptor-1-Mediated Chemoresistance Through Inhibiting S1PR1/P-STAT3 Axis in Ovarian Carcinoma [ Int J Nanomedicine, 2020, 15:5561-5571] PubMed: 32801704
Ponesimod suppresses hepatitis B virus infection by inhibiting endosome maturation [ Antiviral Res, 2020, S0166-3542(20)30413-7] PubMed: 33346055
Siponimod (BAF312) Activates Nrf2 While Hampering NFκB in Human Astrocytes, and Protects From Astrocyte-Induced Neurodegeneration. [ Front Immunol, 2020, 8;11:635] PubMed: 32322257
Sphingosine-1-phosphate signalling drives an angiogenic transcriptional programme in diffuse large B cell lymphoma [ Leukemia, 2019, 10.1038/s41375-019-0478-9] PubMed: 31097785

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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