220619-73-8
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- CAS号:
- 220619-73-8
- 英文名:
- VTP 194204
- 英文别名:
- IRX-4204;NRX-4204;iso IRX-A;NRX 194204;VTP 194204;AGN194204,AGN-194204;AGN194204/IRX4204/NRX194204/VTP 194204);NRX 194204 - NRX 4204/ VTP 194204/ AGN 194204/ AGN 4204;2,4-Pentadienoic acid, 3-methyl-5-[(1S,2S)-2-methyl-2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)cyclopropyl]-, (2E,4E)-
- 中文名:
- 220619-73-8
- 中文别名:
- 化合物 T14145;IRX4204; NRX194204; VTP 194204
- CBNumber:
- CB52667435
- 分子式:
- C24H32O2
- 分子量:
- 352.51
- MOL File:
- 220619-73-8.mol
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220619-73-8化学性质
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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220619-73-8性质、用途与生产工艺
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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RXRα
0.4 nM (Kd)
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RXRβ
3.6 nM (Kd)
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RXRγ
3.8 nM (Kd)
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RXRα
0.2 nM (EC
50
)
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RXRβ
0.8 nM (EC
50
)
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RXRγ
0.08 nM (EC
50
)
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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
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Cell Line:
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SK-BR-3 human breast cancer cells
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Concentration:
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1 μM
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Incubation Time:
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72 hours
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Result:
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Induced apoptosis in lung and breast cancer cells.
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Western Blot Analysis
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Cell Line:
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E, RAW cells
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Concentration:
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0 nM, 1 nM, 10 nM and 100 nM
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Incubation Time:
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24 hours
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Result:
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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.
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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.
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Animal Model:
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Female A/J mice with vinyl carbamate
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Dosage:
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30 mg/kg, 60 mg/kg
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Administration:
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Oral administration; daily; for 15 weeks
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Result:
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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.
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220619-73-8
上下游产品信息
上游原料
下游产品
220619-73-8, 220619-73-8 相关搜索:
- 抑制剂
- IRX4204; NRX194204; VTP 194204
- 化合物 T14145
- 220619-73-8
- AGN194204/IRX4204/NRX194204/VTP 194204)
- AGN194204,AGN-194204
- IRX-4204
- 2,4-Pentadienoic acid, 3-methyl-5-[(1S,2S)-2-methyl-2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)cyclopropyl]-, (2E,4E)-
- iso IRX-A
- NRX 194204 - NRX 4204/ VTP 194204/ AGN 194204/ AGN 4204
- NRX 194204
- VTP 194204
- NRX-4204