AGN194204 (Synonyms: IRX4204; NRX194204; VTP 194204)
目录号: PL10816 纯度: ≥99.0%
CAS No. :220619-73-8
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中文名称
AGN194204
中文别名
(2E,4E)-3-Methyl-5-[(1S,2S)-2-methyl-2-(5,5,8,8-tetramethyl-5,6,7 ,8-tetrahydro-2-naphthalenyl)cyclopropyl]-2,4-pentadienoic acid
英文名称
AGN194204
英文别名
(2e,4e)-3-methyl-5-[(1s,2s)-2-methyl-2-(5,5,8,8-tetramethyl-5,6,7 ,8-tetrahydro-2-naphthalenyl)cyclopropyl]-2,4-pentadienoic Acid;AGN-194204;AGN194204
Cas No.
220619-73-8
分子式
C24H32O2
分子量
352.52
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
AGN194204 (IRX4204) is an orally active and selective RXR agonist with K d values 0.4 nM, 3.6 nM and 3.8 nM and EC 50 s 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.
性状
Solid
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.
AGN194204 (NRX194204; 1 μM; 72 hours; SK-BR-3 human breast cancer cells) treatment induces apoptosis in breast cancer cells. has not independently confirmed the accuracy of these methods. They are for reference only.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
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
ClinicalTrial
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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2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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