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Submit Review(±)-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).
(±)-ML 209 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 441.52 |
公式 | C25H31NO6 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1334526-14-5 |
PubChem ID | 53385590 |
InChI Key | YEKVAIMYYCZDLI-MCPYQZEQSA-N |
Smiles | COC1=CC(OC)=C(C(O)=C1)C(C2=CC=C3OCOC3=C2)CC(N4C[C@@H](C[C@@H](C4)C)C)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 44.15 | 100 |
以下数据基于产品分子量 441.52。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.26 mL | 11.32 mL | 22.65 mL |
5 mM | 0.45 mL | 2.26 mL | 4.53 mL |
10 mM | 0.23 mL | 1.13 mL | 2.26 mL |
50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
参考文献是支持产品生物活性的出版物。
Huang et al (2010) Identification of Potent and Selective RORγ Antagonists. Probe Reports from the NIH Molecular Libraries Program PMID: 23658948
Huang et al (2015) DDX5 and its associated lncRNA Rmrp modulate TH17 cell effector functions. Nature 528 517 PMID: 26675721
Kojetin et al (2014) REV-ERB and ROR nuclear receptors as drug targets. Nat.Rev.Drug Discov. 13 197 PMID: 24577401
Wang et al (2014) Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent RORγt inhibitors. Bioorg.Med.Chem. 22 692 PMID: 24388993
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