AGN 193109

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Chemical Structure| 171746-21-7 同义名 : -
CAS号 : 171746-21-7
货号 : A964784
分子式 : C28H24O2
纯度 : 99%+
分子量 : 392.489
MDL号 : MFCD00943817
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
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：
生物活性
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.
实验方案
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
参考文献

[1]Agarwal C, Chandraratna RA, Johnson AT, Rorke EA, Eckert RL. AGN193109 is a highly effective antagonist of retinoid action in human ectocervical epithelial cells. J Biol Chem. 1996 May 24;271(21):12209-12. doi: 10.1074/jbc.271.21.12209. PMID: 8647816.

[2]Kochhar DM, Jiang H, Penner JD, Johnson AT, Chandraratna RA. The use of a retinoid receptor antagonist in a new model to study vitamin A-dependent developmental events. Int J Dev Biol. 1998 May;42(4):601-8. PMID: 9694631.