A modulator of RORγ and LXR receptors; an inverse agonist of RORγ (IC50 = ~100 nM) and an agonist of LXR; binds to PPARγ (IC50 = 209 nM) but does not activate it; inhibits LPS-induced expression of TREM-1 in RAW 264.7 cells at 10 μM; inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1

SR 1903 – 10 mg

Brand:
Cayman
CAS:
1414248-06-8
Storage:
-20
UN-No:
Non-Hazardous - /

SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).{35980} It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg/kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.  

 

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SKU: 28253 - 10 mg Category:

Description

A modulator of RORγ and LXR receptors; an inverse agonist of RORγ (IC50 = ~100 nM) and an agonist of LXR; binds to PPARγ (IC50 = 209 nM) but does not activate it; inhibits LPS-induced expression of TREM-1 in RAW 264.7 cells at 10 μM; inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells; reduces severity score in a mouse model of collagen-induced arthritis at 20 mg/kg twice per day; reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity

Formal name: 2′-methyl-4′-[[4-(4-pyridinylmethyl)-1-piperazinyl]methyl]-α,α-bis(trifluoromethyl)-[1,1′-biphenyl]-4-methanol

Synonyms: 

Molecular weight: 523.5

CAS: 1414248-06-8

Purity: ≥98%

Formulation: A crystalline solid

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