AGN 193109 is a high affinity pan-retinoic acid receptor (RAR) antagonist with Kds of 2, 2 and 3 nM at RARα, RARβ and RARγ, respectively.
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描述 | Retinoic acid is an active metabolite of vitamin A that plays an important role in cell growth and embryonic development. It interacts with retinoic acid receptor (RAR) and retinoic acid X receptor (RXR) to regulate gene expression. AGN 193109 is an antagonist of RAR, which binds to RARα, RARβ, and RAR with Kd values of 2, 2, and 3 nM, respectively. However, it was unable to bind to RXR. AGN 193109 at 100 nM inhibited TTNPB-induced morphological change in ECE16-1 cells. The TTNPB-dependent suppression of ECE16-1 cell proliferation was reserved by AGN 193109 at the doses of 10 - 100 nM. Treatment with AGN 193109 alone (1 μΜ) showed no effect on cell proliferation in ECE16-1 cells. TTNPB at 10 nM suppressed the levels of cytokeratins K5, K6, K14, K16, and K17 and elevated the expressions of K7, K8, and K19. Simultaneous treatment with AGN193109 (100 nM) eliminates TTNPB-induced changes of these retinoid-responsive marker genes[1]. In pregnant mice, a single oral dose of AGN 193109 (1 mg/kg) induced a severe craniofacial anomaly and eye malformations in all fetuses[2]. |
作用机制 | AGN193109 is an effective RAR antagonist that binds to all three RAR subtypes with high affinities. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.55mL 0.51mL 0.25mL |
12.74mL 2.55mL 1.27mL |
25.48mL 5.10mL 2.55mL |
CAS号 | 171746-21-7 |
分子式 | C28H24O2 |
分子量 | 392.489 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 2 mg/mL(5.1 mM),配合水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |