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Technical Data
| Formula | C15H13F6N3O4S2 |
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| Molecular Weight | 477.40 | CAS No. | 1335106-03-0 | |
| Solubility (25°C)* | In vitro | DMSO | 95 mg/mL (198.99 mM) | |
| Ethanol | 95 mg/mL (198.99 mM) | |||
| Water | Insoluble | |||
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* <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.) |
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Biological Activity
| Description | SR1001 is a RORα inverse agonist with Ki values of 172 nM and 111 nM for RORα and RORγ respectively. | ||||
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| Targets |
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| In vitro | SR1001 binds specifically to the ligand binding domains (LBDs) of RORα and RORγt inducing a conformational change within the LBD that encompasses repositioning of helix 12 leading to diminished affinity for coactivators and increased affinity for corepressors resulting in suppression of the receptors transcriptional activity[2]. |
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| In vivo | SR1001 suppresses the immune response, including TH17 cells in vitro and in vivo, TH1 cells in vivo, autoantibody production, maintains insulin levels, and increases Foxp3 expression[1]. SR1001 effectively protects against pathologic neovascularization in both oxygen-induced retinopathy and another angiogenic model of very-low-density lipoprotein receptor (Vldlr)-deficient (Vldlr −/−) mice with spontaneous subretinal neovascularization[3]. |
Protocol (from reference)
| Animal Study: |
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References
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RETURN POLICY
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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.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.