VAF347
目录号 : GC61367
VAF347是一种细胞可渗透且高度亲和力的芳烃受体(AhR)激动剂,可诱导AhR信号传导。VAF347抑制颗粒单核细胞(GM期)前体中CD14+CD11b+单核细胞的发育。VAF347具有抗炎作用。
Cas No.:574759-62-9
Sample solution is provided at 25 µL, 10mM.
VAF347 is a cell permeable and highly affinity aryl hydrocarbon receptor (AhR) agonist and induces AhR signaling. VAF347 inhibits the development of CD14+CD11b+ monocytes from granulo-monocytic (GM stage) precursors. VAF347 has anti-inflammatory effects[1].
VAF347 (0.01-20 μM; 48-72 hours; HL-60 cells) treatment enhances retinoic acid-induced cell cycle arrest[1].VAF347 (20 μM; 48 hours; HL-60 cells) treatment augments retinoic acid-induced expression of AhR, Lyn, Vav1, and c-Cbl as well as p47phox. Several interactions of partners in the signalsome appear to be enhanced: Fgr interaction with c-Cbl, CD38, and with pS259c-Raf and AhR interaction with c-Cbl and Lyn[1].VAF347 inhibits IL-4+ GM-CSF induced IL-6 production in MM1 cells with an IC50 of ~5 nM[2]. Cell Cycle Analysis[1] Cell Line: HL-60 cells
In wild-type mice, VAF347 treatment leads to a strong reduction of total serum IgE levels compared with vehicle-treated animals. IL-5 levels in the bronchoalveolar fluid are inhibited to a comparable degree. AhR-deficient mice are resistant to the VAF347's ability to block allergic lung inflammation in vivo[2].
[1]. Ibabao CN, et al. The AhR agonist VAF347 augments retinoic acid-induced differentiation in leukemia cells. FEBS Open Bio. 2015 Apr 8;5:308-18. [2]. B Paige Lawrence, et al. Activation of the aryl hydrocarbon receptor is essential for mediating the anti-inflammatory effects of a novel low-molecular-weight compound. Blood. 2008 Aug 15;112(4):1158-65.
Cas No. | 574759-62-9 | SDF | |
Canonical SMILES | FC(C1=CC=C(NC2=NC=CC(C3=CC=CC(Cl)=C3)=N2)C=C1)(F)F | ||
分子式 | C17H11ClF3N3 | 分子量 | 349.74 |
溶解度 | DMSO : 31.25 mg/mL (89.35 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
1 mM | 2.8593 mL | 14.2963 mL | 28.5927 mL |
5 mM | 0.5719 mL | 2.8593 mL | 5.7185 mL |
10 mM | 0.2859 mL | 1.4296 mL | 2.8593 mL |
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >99.50%
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