AGN194204(Synonyms: IRX4204; NRX194204; VTP 194204)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

AGN194204 (Synonyms: IRX4204; NRX194204; VTP 194204) 纯度: ≥99.0%

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。

AGN194204(Synonyms: IRX4204; NRX194204; VTP 194204)

AGN194204 Chemical Structure

CAS No. : 220619-73-8

规格 价格 是否有货 数量
1 mg ￥5000 In-stock
5 mg ￥9500 In-stock
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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[1][2].

IC50 & Target

RXRα

0.4 nM (Kd)

RXRβ

3.6 nM (Kd)

RXRγ

3.8 nM (Kd)

RXRα

0.2 nM (EC50)

RXRβ

0.8 nM (EC50)

RXRγ

0.08 nM (EC50)

体外研究
(In Vitro)

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[1].
AGN194204 (NRX194204; 1 μM; 72 hours; SK-BR-3 human breast cancer cells) treatment induces apoptosis in breast cancer cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

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[1]

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
(In Vivo)

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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female A/J mice with vinyl carbamate[1]
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.

Clinical Trial

分子量

352.51

Formula

C24H32O2
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
参考文献

  • [1]. Liby K, et al. A new rexinoid, NRX194204, prevents carcinogenesis in both the lung and mammary gland. Clin Cancer Res. 2007 Oct 15;13(20):6237-43.

    [2]. Vuligonda V, et al. Enantioselective syntheses of potent retinoid X receptor ligands: differential biological activities of individual antipodes. J Med Chem. 2001 Jul 5;44(14):2298-303.

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