AGN194204  ≥98%

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包装规格:1mg in glass bottle
产品描述:基本信息 产品编号: A11301 产品名称: AGN194204 CAS: 220619-73-8   储存条件 粉末 -20℃ 四年     分子式: C24H32O2 溶于液体 -80℃ 六个月 分子量 352.51 -20℃ 一个月 化学名:  3-Methyl-5-[2-methyl-2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-cyclopropyl]-penta-2,4-dienoic acid   生物活性 产品描述 一种具有口服活性的,选择性RXR激动剂,对RXRα,RXRβ和RXRγ的Kd值分别为0.4nM,3.6nM和3.8nM,EC50分别为0.2nM,0.8nM和0.08nM。 靶点 RXRα 0.4nM(Kd) RXRβ 3.6nM(Kd) RXRγ 3.8nM(Kd) RXRα 0.2nM(EC50) RXRβ 0.8nM(EC50) RXRγ 0.08nM(EC50) 体外研究 AGN194204 (NRX194204; 0-100nM; 24 hours; E, RAW cells) treatment blocks the ability of lipopolysaccharide and tumor necrosis factor-α to induce the release of nitric oxide and interleukin 6 and the degradation of IKBα in RAW264.7 macrophage-like cells. AGN194204 (NRX194204; 1μM; 72 hours; SK-BR-3 human breast cancer cells) treatment induces apoptosis in breast cancer cells Apoptosis Analysis Cell Line: SK-BR-3 human breast cancer cells Concentration: 1μM Incubation Time: 72 hours Result: Induced apoptosis in lung and breast cancer cells. Western Blot Analysis Cell Line: E, RAW cells Concentration: 0nM, 1nM, 10nM and 100nM Incubation Time: 24 hours Result: Blocked the ability of lipopolysaccharide and tumor necrosis factor-α to induce the release of nitric oxide and interleukin 6 and the degradation of IKBα in RAW264.7 macrophage-like cells. 体内研究 AGN194204 (NRX194204; 30-60mg/kg; oral administration; daily; for 15 weeks; female A/J mice) treatment significantly reduces the number and size of tumors on the surface of the lungs and reduces the total tumor volume per slide by 64% to 81% compared with the control group Animal Model: Female A/J mice with vinyl carbamate Dosage: 30mg/kg, 60mg/kg Administration: Oral administration; daily; for 15 weeks Result: Significantly reduced the number and size of tumors on the surface of the lungs and reduced the total tumor volume per slide by 64% to 81% compared with the control group.
保存条件:-20℃