220619-73-8
- CAS号:220619-73-8
- 英文名:VTP 194204
- 中文名:220619-73-8
- CBNumber:CB52667435
- 分子式:C24H32O2
- 分子量:352.51
- MOL File:220619-73-8.mol
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
- 形态 :Solid
- 颜色 :White to off-white
220619-73-8性质、用途与生产工艺
- 生物活性 AGN194204 (IRX4204) 是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 0.4 nM,3.6 nM 和 3.8 nM,EC50 分别为 0.2 nM,0.8 nM 和 0.08 nM。AGN194204 对 RAR 无活性,并具有抗炎和抗癌作用。
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靶点
RXRα
0.4 nM (Kd)
RXRβ
3.6 nM (Kd)
RXRγ
3.8 nM (Kd)
RXRα
0.2 nM (EC 50 )
RXRβ
0.8 nM (EC 50 )
RXRγ
0.08 nM (EC 50 )
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体外研究
AGN194204 (NRX194204; 0-100 nM; 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; 1 μM; 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: 1 μM Incubation Time: 72 hours Result: Induced apoptosis in lung and breast cancer cells. Western Blot Analysis
Cell Line: E, RAW cells Concentration: 0 nM, 1 nM, 10 nM and 100 nM 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; 30-60 mg/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: 30 mg/kg, 60 mg/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.
- 公司名称:CLEARSYNTH LABS LTD.
- 联系电话:--
- 电子邮件:sales@clearsynth.com
- 国家:印度
- 产品数:6351
- 优势度:58