A synthetic ligand specific for RORα and RORγ (Kis = 172 and 111 nM

SR 1001 – 25 mg

Brand:
Cayman
CAS:
1335106-03-0
Storage:
-20
UN-No:
Non-Hazardous - /

Retinoic-acid-receptor-related orphan receptors (ROR) α and γ play a key role in the development of T-helper cells that produce interleukin-17 (TH17 cells), a subset of CD4+ T-cells that contribute to the inflammatory process and have been implicated in the pathology of autoimmune diseases. SR 1001 is a synthetic ligand specific for RORα and RORγ (Kis = 172 and 111 nM, respectively) that functions as an inverse agonist at these receptors.{19493} SR 1001 has been shown to suppress IL-17 promoter driven transcriptional activity by inhibiting the interaction of co-activators such as TRAP220 nuclear receptor box 2 peptide (IC50 = 117 nM) and SRC2 with RORα and RORγ as well as by increasing the recruitment of corepressors such as NCoR. At 5 μM, SR 1001 inhibits TH17 cell differentiation and IL-17A secretion in cultured splenocytes and human PBMCs. A 25 mg/kg dose of SR 1001 twice/day delays the onset and the severity of experimental autoimmune encephalomyelitis, a mouse model of multiple sclerosis.{19493}  

 

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SKU: 10922 - 25 mg Category:

Description

A synthetic ligand specific for RORα and RORγ (Kis = 172 and 111 nM, respectively) that functions as an inverse agonist; inhibits TH17 cell differentiation and IL-17A secretion in cultured splenocytes and human PBMCs at 5 μM; 25 mg/kg twice/day delays onset and severity of experimental autoimmune encephalomyelitis, a mouse model of multiple sclerosis

Formal name: N-(5-(N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)sulfamoyl)-4-methylthiazol-2-yl)acetamide

Synonyms: 

Molecular weight: 477.4

CAS: 1335106-03-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Autoimmunity||Research Area|Immunology & Inflammation|Innate Immunity

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