SR 2211
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SR 2211是一种有效的和选择性的RORγ反向激动剂,IC50值为320 nM[1]。
RAR相关孤儿受体γ(RORγ)是一种核受体和DNA结合转录因子。RORγ在调节昼夜节律及Th17细胞的分化中起重要作用[2]。
SR 2211是一种有效的和选择性的RORγ反向激动剂。SR2211与RORγ结合,Ki值为105 nM。SR2211(10 μM)抑制90%的RORγ活性,而不影响RORα和法尼醇X受体(FXR)的转录活性。SR2211可微弱激活肝X受体α(LXRα)。在EL-4小鼠T淋巴细胞的细胞系中,SR2211(5 μM)之后用PMA/ionomycin处理可显著抑制IL-17和IL-23受体的表达,呈现剂量依赖的方式[1]。在Th17极化条件下的丰富naive CD4+ T细胞中,SR2211显著抑制IL-17的产生,表明SR2211抑制Th17细胞分化。在LPS刺激的RAW 264.7细胞中,SR2211(5 μM)抑制TNFα、IL-1β和IL-6的表达,它们都是促炎细胞因子,在关节炎(RA)的发病中扮演重要作用[2]。
在CIA小鼠模型中,SR2211(20 mg/kg)以剂量依赖的方式抑制关节炎的发展[2]。
参考文献:
[1]. Kumar N, Lyda B, Chang MR, et al. Identification of SR2211: a potent synthetic RORγ-selective modulator. ACS Chem Biol, 2012, 7(4): 672-677.
[2]. Chang MR, Lyda B, Kamenecka TM, et al. Pharmacologic Repression of Retinoic Acid Receptor-Related Orphan Nuclear Receptor γ Is Therapeutic in the Collagen-Induced Arthritis Experimental Model. Arthritis Rheumatol, 2014, 66(3): 579-588.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 527.48 |
Cas No. | 1359164-11-6 |
Formula | C26H24F7N3O |
Solubility | Soluble in DMSO |
Chemical Name | 1,1,1,3,3,3-hexafluoro-2-(2-fluoro-4'-((4-(pyridin-4-ylmethyl)piperazin-1-yl)methyl)-[1,1'-biphenyl]-4-yl)propan-2-ol |
SDF | Download SDF |
Canonical SMILES | FC1=CC(C(C(F)(F)F)(C(F)(F)F)O)=CC=C1C2=CC=C(C=C2)CN3CCN(CC4=CC=NC=C4)CC3 |
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