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220619-73-8

中文名稱 220619-73-8
英文名稱 VTP 194204
CAS 220619-73-8
分子式 C24H32O2
分子量 352.51
MOL 文件 220619-73-8.mol
220619-73-8 結(jié)構(gòu)式 220619-73-8 結(jié)構(gòu)式

基本信息

中文別名
化合物 T14145
IRX4204
NRX194204
VTP 194204
英文別名
NRX-4204
IRX-4204
iso IRX-A
NRX 194204
VTP 194204
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)-

物理化學性質(zhì)

儲存條件-20°C儲存
溶解度溶于二甲基亞砜
形態(tài)Solid
顏色White to off-white

常見問題列表

生物活性
AGN194204 (IRX4204) 是一種具有口服活性的,選擇性 RXR 激動劑,對 RXRα,RXRβ 和 RXRγ 的 Kd 值分別為 0.4 nM,3.6 nM 和 3.8 nM,EC50 分別為 0.2 nM,0.8 nM 和 0.08 nM。AGN194204 對 RAR 無活性,并具有抗炎和抗癌作用。
靶點

RXRα

0.4 nM (Kd)

RXRβ

3.6 nM (Kd)

RXRγ

3.8 nM (Kd)

RXRα

0.2 nM (EC 50 )

RXRβ

0.8 nM (EC 50 )

RXRγ

0.08 nM (EC 50 )

體外研究

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.
體內(nèi)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.
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