AGN194204 (Synonyms:IRX4204; NRX194204; VTP 194204)
目录号 : KM11097 CAS No. : 220619-73-8 纯度 : 98%

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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生物活性

AGN194204 (IRX4204) is an orally active and selective RXR agonist with Kd values 0.4 nM, 3.6 nM and 3.8 nM and EC50s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα, RXRβ and RXRγ, respectively. AGN194204 is inactive against RAR. AGN194204 has anti-inflammatory and anticarcinogenic actions.

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.
分子式
C24H32O2
分子量
352.51
CAS号
220619-73-8
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
临床试验
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