CH-223191

发表于由

CH-223191

货号：
IC3880

品牌：
Jinpan

CH-223191

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CH-223191

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产品简介
有效期 2年
MDL MFCD00377884
英文名称 CH-223191
CAS 301326-22-7
分子式 C19H19N5O
分子量 333.39
储存条件 2-8℃
纯度 ≥98%
外观（性状） Off-white to orange Powder
单位 瓶
In Vitro CH-223191阻断TCDD介导的核易位以及AhR 的DNA结合，也会抑制TCDD诱导的细胞色素P450酶活性。[1]在人恶性胶质瘤细胞中，CH-223191下调TGF-β/ Smad信号通路，并减少克隆存活和侵染力。[2]在SK-N-SH人衍生的神经元细胞中，CH223191抵消TCDD诱导的对神经元乙酰胆碱酯酶表达的抑制。[3]在内皮细胞中，CH-223191增强ICAM-1表达，并防止RelB核易位。[4]
In Vivo CH-223191 (10 mg/kg/day, p.o.)有效预防小鼠体内TCDD引起的细胞色素P450诱导，肝毒性，和消耗综合症。[1]
激酶实验 The ability of CH-223191 to compete with TCDD for binding to the AhR was assessed by incubating aliquots of cytosol prepared from untreated Hepa cells (2.1–2.5 mg protein/ml) with CH-223191 or flavone and [3H]TCDD at 3 nM for 2 h at room temperature. This concentration of TCDD is nonsaturating at these protein concentrations. Specific binding of [3H]TCDD was determined in duplicate aliquots by the hydroxylapatite assay(Gasiewicz and Neal, 1982), with correction for nonspecific binding measured in the presence of 150-fold excess of unlabeled 2,3,7,8-tetrachlorodibenzofuran. Data were expressed for each antagonist concentration as a percentage of the specific binding of [3H]TCDD in the absence of competitor.[1]
SMILES O=C(C1=CC=NN1C)NC2=CC=C(/N=N/C3=CC=CC=C3C)C=C2C
靶点 Aryl Hydrocarbon Receptor(AhR)
动物实验 Male ICR mice (6 weeks old) were given oral vehicle (corn oil) or CH-223191 (10 mg/kg in corn oil) once a day for 25 days and treated i.p. with TCDD (100 g/kg in corn oil) once after the first week of CH-223191 treatment. The body weights of all mice were measured before dosing and at termination.[1]
数据来源文献 [1] Kim SH, et al. Mol Pharmacol. 2006, 69(6), 1871-1878.
[2] Gramatzki D, et al. Oncogene. 2009, 28(28), 2593-2605.
[3] Xie HQ, et al. Environ Health Perspect. 2013, 121(5), 613-618.
[4] de Souza AR, et al. Toxicol Sci. 2014, 140(1), 204-223.
规格 5mg 10mg

是一种有效的特定aryl hydrocarbon receptor (AhR)拮抗剂。