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Formula | C29H35F3N2O3 |
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Molecular Weight | 516.6 | CAS No. | 1230487-00-9 | |
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (193.57 mM) | |
Ethanol | 44 mg/mL (85.17 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | BAF312 (Siponimod) is a next-generation S1P receptor agonist, 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. | ||||
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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] |
Kinase Assay:[1] |
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Cell Assay: [1] |
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Animal Study:[1] |
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Data from [Data independently produced by , , Leukemia, 2018, 32(1):214-223]
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 |
An essential role forsphingosine1-phosphate in oligodendrocyte survival and remyelination [ , 2021, ] | PubMed: none |
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 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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