(±)-ML 209
Chemical Name: 3-(1,3-Benzodioxol-5-yl)-1-(cis-3,5-dimethyl-1-piperidinyl)-3-(2-hydroxy-4,6-dimethoxyphenyl)-1-propanone
Purity: ≥98%
Biological Activity
(±)-ML 209 is a RORγt inverse agonist (IC50 = 460 nM). Suppresses Th17 cell differentiation and IL17A expression in vitro. Does not suppress transcription of RORα. Minimal activity displayed on ERα, LXRα and thyroid hormone receptors (IC50 values >4.4 μM).Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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DDX5 and its associated lncRNA Rmrp modulate TH17 cell effector functions.
Huang et al.
Nature, 2015;528:517 -
REV-ERB and ROR nuclear receptors as drug targets.
Kojetin et al.
Nat.Rev.Drug Discov., 2014;13:197 -
Identification of Potent and Selective RORγ Antagonists.
Huang et al.
Probe Reports from the NIH Molecular Libraries Program, 2010; -
Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent RORγt inhibitors.
Wang et al.
Bioorg.Med.Chem., 2014;22:692
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