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AGN194204
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AGN194204图片
CAS NO:220619-73-8
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品名称
IRX4204
NRX194204
VTP 194204
产品介绍
AGN194204 (IRX4204) 是一种具有口服活性的,选择性RXR激动剂,对RXRαRXRβRXRγKd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 selectiveRXRagonist withKdvalues 0.4 nM, 3.6 nM and 3.8 nM andEC50s of 0.2 nM, 0.8 nM and 0.08 nM forRXRα,RXRβandRXRγ, respectively. AGN194204 is inactive against RAR. AGN194204 has anti-inflammatory and anticarcinogenic actions[1][2].

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].

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].

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

性状

Solid

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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month