4-[2-[5,6-二氢-5,5-二甲基-8-(4-甲基苯基)-2-萘基]乙炔基]苯甲酸
中文名称 | 4-[2-[5,6-二氢-5,5-二甲基-8-(4-甲基苯基)-2-萘基]乙炔基]苯甲酸 |
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中文同义词 | 4-[2-[5,6-二氢-5,5-二甲基-8-(4-甲基苯基)-2-萘基]乙炔基]苯甲酸;4-[2-[5,6-二氢-5,5-二甲基-8-(4-甲基苯基)-2-萘基]炔基]苯甲酸;化合物AGN 193109;AGN 193109,泛RAR拮抗剂 |
英文名称 | 4-{[5,5-dimethyl-8-(4-methylphenyl)-5,6-dihydronaphthalen-2-yl]ethynyl}benzoic acid |
英文同义词 | AGN 193109;4-[2-[5,6-Dihydro-5,5-dimethyl-8-(4-methylphenyl)-2-naphthalenyl]ethynyl]benzoic Acid;CD 3106;4-((5,5-Dimethyl-8-p-tolyl-5,6-dihydronaphthalen-2-yl)ethynyl)benzoic acid;4-{[5,5-diMethyl-8-(4-Methylphenyl)-5,6-dihydronaphthalen-2-yl]ethynyl}benzoic acid;AGN 193109 SodiuM Salt;Benzoic acid, 4-[2-[5,6-dihydro-5,5-dimethyl-8-(4-methylphenyl)-2-naphthalenyl]ethynyl]-;AGN193109,Autophagy,Inhibitor,Retinoic acid receptors,Retinoid X receptors,RAR/RXR,AGN 193109,AGN-193109,inhibit |
CAS号 | 171746-21-7 |
分子式 | C28H24O2 |
分子量 | 392.49 |
EINECS号 | |
相关类别 | Aromatics Compounds;Aromatics;Intermediates & Fine Chemicals;Pharmaceuticals |
Mol文件 | 171746-21-7.mol |
结构式 |
4-[2-[5,6-二氢-5,5-二甲基-8-(4-甲基苯基)-2-萘基]乙炔基]苯甲酸 性质
熔点 | 246-255?C |
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沸点 | 564.5±50.0 °C(Predicted) |
密度 | 1.21±0.1 g/cm3(Predicted) |
储存条件 | Sealed in dry,Store in freezer, under -20°C |
溶解度 | 可溶于氯仿(轻微加热)、DMSO(轻微超声处理) |
形态 | 固体 |
酸度系数(pKa) | 4.08±0.10(Predicted) |
颜色 | 灰白色至浅黄色 |
稳定性 | 吸湿性 |
Kd: 2 nM (RARα), 2 nM (RARβ), 3 nM (RARγ)
AGN 193109 is a highly effective antagonist of retinoic acid receptors, with K d s 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. 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.
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-U00449 | AGN 193109 | 1 mg | 863元 | |
2024/08/19 | HY-U00449 | 4-[2-[5,6-二氢-5,5-二甲基-8-(4-甲基苯基)-2-萘基]乙炔基]苯甲酸 AGN 193109 | 171746-21-7 | 5mg | 1900元 |