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MedChemExpressModel SR-1903 -1414248-06-8

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SR-1903 is an inverse agonist of RORγ and PPARγ (IC50 of ∼100 nM and 209 nM for RORγ and PPARγ, respectively) and a LXR agonist. SR-1903 exhibits anti-inflammatory and anti-diabetic efficacy in collagen-induced arthritis and diet-induced obesity mouse models[1].
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SR-1903

MCE China:SR-1903

Brand:MedChemExpress (MCE)

Cat. No.HY-138007

CAS:1414248-06-8

Storage:Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping:Room temperature in continental US; may vary elsewhere.

Description:SR-1903 is an inverse agonist of RORγ and PPARγ (IC50 of ∼100 nM and 209 nM for RORγ and PPARγ, respectively) and a LXR agonist. SR-1903 exhibits anti-inflammatory and anti-diabetic efficacy in collagen-induced arthritis and diet-induced obesity mouse models.

In Vitro:SR1903 (10 μM) attenuates LPS (HY-D1056) signaling in macrophages, with suppression of TREM-1 gene expression[1]. SR1903 increases expression of LXR target genes, including genes involved in macrophage cholesterol efflux (ABCG1 and SCD) and lipid metabolism (ACACA and FASN) in macrophage RAW264.7[1].

In Vivo:SR1903 (20 mg/kg, i.p., twice-a-day for a total of 16 days) ameliorates arthritic symptoms and prevents thymocyte loss in collagen-induced arthritis (CIA) mice[1]. SR1903 (20 mg/kg, i.p., 14 days) improves metabolic parameters and protects against obesity-associated thymic degeneration in diet-induced obese (DIO) mice[1].

IC50 & Target:RORγ ~100 nM (IC50) PPARγ 209 nM (IC50)

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References:

[1]. Chang MR, et al. Unique Polypharmacology Nuclear Receptor Modulator Blocks Inflammatory Signaling Pathways. ACS Chem Biol. 2019, 14(5):1051-1062.  [Content Brief]

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