9-顺式视黄酸

9-顺式视黄酸用途

9-cis-Retinoic acid (ALRT1057),维生素 A 的衍生物,是一种有效的 RAR/RXR 激动剂。9-cis-Retinoic acid 可诱导细胞凋亡 (apoptosis),调节细胞周期并具有抗癌,抗炎和神经保护活性。

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9-顺式视黄酸名称

[ CAS 号 ]:
5300-03-8

[ 中文名 ]:
9-顺式视黄酸

[ 英文名 ]:
Alitretinoin

[中文别名 ]:

[英文别名 ]:

9-cis-Tretinoin,Alitretinoin
(9cis)-Retinoic acid
Alitretinoin
9-cis-retinoic acid
MFCD00270072
9Z-retinoic acid
9-cis-Tretinoin
9-cis Retinoic Acid
Panretin Gel
Retinoic acid, (9cis)-

9-顺式视黄酸生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

研究领域 >> 炎症/免疫

研究领域 >> 神经疾病

信号通路 >> 代谢酶/蛋白酶 >> RAR/RXR

[体外研究]

9-顺式维甲酸(1-10μM；0-5天；Ca9-22和NA细胞)处理显著降低Ca9-22和NA细胞的增殖,呈剂量依赖性[1]。9-顺式维甲酸(1μM；24小时)处理可显著提高CA 9-22和NA空气消化细胞的PPARγ功能活性>200%。9-顺式维甲酸处理导致CA 9-22细胞形成核PPARγ-RXRα异二聚体超转移复合物[1]。9-顺式维甲酸抑制皮肤T细胞淋巴瘤(CTCL)增殖,诱导细胞凋亡,呈剂量依赖性和时间依赖性。9-顺式维甲酸也通过下调细胞周期蛋白D1诱导G0/G1细胞周期阻滞。9-顺式维甲酸显著降低JAK1、STAT3和STAT5的磷酸化,下调Bcl-xL和cyclin D1[2]。细胞增殖试验[1]细胞株：ca9-22,NA细胞浓度：1μM,10μM孵育时间：0天、1天、3天、5天结果：细胞增殖明显下降。

[体内研究]

9-顺式维甲酸(1mg/kg；静脉注射；每日；连续10天；雄性C57BL/6J小鼠)治疗显著降低血清ALT和AST水平,减轻胆管结扎(BDL)小鼠肝脏坏死[3]。动物模型：雄性C57BL/6J小鼠(6-8周；19-22g)结扎胆管治疗[3]剂量：1mg/kg给药：静脉注射；每日；10天结果：显著降低血清ALT和AST水平,减轻肝坏死。

[参考文献]

[1]. Raul Rosas, et al. Retinoids Augment Thiazolidinedione PPARγ Activation in Oral Cancer Cells. Anticancer Res. 2020 Jun;40(6):3071-3080.

[2]. Hua Yang, et al. Effects of 9-cis-retinoic Acid on the Proliferation and Apoptosis of Cutaneous T-cell Lymphoma Cells. Anticancer Drugs. 2019 Jan;30(1):56-64.

[3]. Zhiqing Yuan, et al. 9-cis-retinoic Acid Elevates MRP3 Expression by Inhibiting Sumoylation of RXRα to Alleviate Cholestatic Liver Injury. Biochem Biophys Res Commun. 2018 Sep 3;503(1):188-194.

[4]. V M Manzano, et al. Human Renal Mesangial Cells Are a Target for the Anti-Inflammatory Action of 9-cis Retinoic Acid. Br J Pharmacol. 2000 Dec;131(8):1673-83.

[5]. Gro H Mathisen, et al. Delayed Translocation of NGFI-B/RXR in Glutamate Stimulated Neurons Allows Late Protection by 9-cis Retinoic Acid. Biochem Biophys Res Commun. 2011 Oct 14;414(1):90-5.

9-顺式视黄酸物理化学性质

[ 密度 ]:
1.0±0.1 g/cm3

[ 沸点 ]:
462.8±14.0 °C at 760 mmHg

[ 熔点 ]:
189-191ºC

[ 分子式 ]:
C₂₀H₂₈O₂

[ 分子量 ]:
300.435

[ 闪点 ]:
350.6±11.0 °C

[ 精确质量 ]:
300.208923

[ PSA ]:
37.30000

[ LogP ]:
6.83

[ 外观性状 ]:
淡黄色固体

[ 蒸汽压 ]:
0.0±2.5 mmHg at 25°C

[ 折射率 ]:
1.556

[ 储存条件 ]:
−20°C

[ 稳定性 ]:
Store Dry in Freezer at -20°C for up to 1 year; in Solution at -20°C for up to 3 Months.

9-顺式视黄酸MSDS

详细MSDS(安全技术说明书)

9-顺式视黄酸安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H315-H319-H335-H360

[ 警示性声明 ]:
P201-P261-P305 + P351 + P338-P308 + P313

[ 个人防护装备 ]:
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R36/37/38;R61

[ 安全声明 (欧洲) ]:
S26-S36/37/39-S45-S53

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ 海关编码 ]:
2916209090

9-顺式视黄酸海关

[ 海关编码 ]: 2916209090

[ 中文概述 ]:
2916209090 其他（环烷、环烯、环萜烯）一元羧酸（包括酸酐、酰卤化物，过氧化物和过氧酸及该税号的衍生物）. 增值税率:17.0% 退税率:9.0% 监管条件:AB(入境货物通关单,出境货物通关单) 最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 丙烯酸、丙烯酸盐或酯应报明包装

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: R.进口食品卫生监督检验 S.出口食品卫生监督检验 M.进口商品检验 N.出口商品检验

[ Summary ]:
2916209090 other cyclanic, cyclenic or cyclotherpenic monocarboxylic acids, their anhydrides, halides, peroxides, peroxyacids and their derivatives VAT:17.0% Tax rebate rate:9.0% Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward) MFN tariff:6.5% General tariff:30.0%

9-顺式视黄酸文献

Modulators of hepatic lipoprotein metabolism identified in a search for small-molecule inducers of tribbles pseudokinase 1 expression.

PLoS ONE 10 , e0120295, (2015)

Recent genome wide association studies have linked tribbles pseudokinase 1 (TRIB1) to the risk of coronary artery disease (CAD). Based on the observations that increased expression of TRIB1 reduces se...

Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.

Chem. Res. Toxicol. 23 , 171-83, (2010)

Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental...

Developmental regulation and induction of cytochrome P450 2W1, an enzyme expressed in colon tumors.

PLoS ONE 10(4) , e0122820, (2015)

Cytochrome P450 2W1 (CYP2W1) is expressed predominantly in colorectal and also in hepatic tumors, whereas the levels are insignificant in the corresponding normal human adult tissues. CYP2W1 has been ...

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