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AGN 193109
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AGN 193109图片
CAS NO:171746-21-7
规格:98%
分子量:392.49
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
AGN193109是一种视黄酸类似物,是有效的,特异性的视黄酸受体(RARs)拮抗剂,可抑制RARα,RARβ和RARγ的活性,Kd值分别为2nM,2nM和3nM。
CAS:171746-21-7
分子式:C28H24O2
分子量:392.49
纯度:98%
存储:Store at -20°C

Background:

AGN 193109 is a retinoid analog, and acts as a specific and highly effective antagonist of retinoic acid receptors (RARs), with Kds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively.


AGN 193109 is a highly effective antagonist of retinoic acid receptors, with Kds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively. AGN 193109 is completely RAR specific, because it does not bind to or transactivate through any of the RXRs[1]. AGN 193109 (100 nM) inhibits the TTNPB (a retinoic acid receptor agonist)-dependent morphological change in ECE16-1 cells. AGN193109 half-reverses retinoid-dependent growth suppression at 10 nM, and completely shows this effect at 100 nM in ECE16-1 cells. AGN193109 (100 nM) also eliminates TTNPB-induced decrease in levels of K5, K6, K14, K16, and K17 and increase in levels of K7, K8, and K19[2].


AGN 193109 (1.15 μmol/kg) does not causes overt toxicity and has no effect on spleen weight on the mice, but it suppresses TTNPB-induced increase in spleen weight of the mice. AGN 193109 also significantly reduces the cutaneous toxicity induced by ATRA. AGN 193109 (0.30 or 1.20 μmol/kg) by topical treatment significantly reduces both weight loss and cutaneous toxicity caused by oral TTNPB cotreatment[3].


[1]. Johnson AT, et al. Synthesis and characterization of a highly potent and effective antagonist of retinoic acid receptors. J Med Chem. 1995 Nov 24;38(24):4764-7. [2]. Agarwal C, et al. AGN193109 is a highly effective antagonist of retinoid action in human ectocervical epithelial cells. J Biol Chem. 1996 May 24;271(21):12209-12. [3]. Standeven AM, et al. Specific antagonist of retinoid toxicity in mice. Toxicol Appl Pharmacol. 1996 May;138(1):169-75.