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Chelerythrine

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Rating icon 很棒

纯度: 99.96%

货号 T6S0052Cas号 34316-15-9

别名 白屈菜红碱, Toddalin, Cheleritrine, Broussonpapyrine

Chelerythrine (Broussonpapyrine) 是一种天然生物碱,为有效、选择性的 Ca2+/磷脂依赖性PKC 拮抗剂,IC50值为 0.7 μM。它具有抗肿瘤、抗糖尿病、抗炎的活性。它抑制BclXL-Bak BH3肽结合,IC50为 1.5 μM,并从 BclXL 取代了 Bax。它诱导细胞凋亡和自噬。

Chelerythrine

Chelerythrine

一键复制产品信息
Rating icon 很棒

纯度: 99.96%

货号 T6S0052 别名 白屈菜红碱, Toddalin, Cheleritrine, BroussonpapyrineCas号 34316-15-9

Chelerythrine (Broussonpapyrine) 是一种天然生物碱,为有效、选择性的 Ca2+/磷脂依赖性PKC 拮抗剂,IC50值为 0.7 μM。它具有抗肿瘤、抗糖尿病、抗炎的活性。它抑制BclXL-Bak BH3肽结合,IC50为 1.5 μM,并从 BclXL 取代了 Bax。它诱导细胞凋亡和自噬。

规格价格库存数量
5 mg
¥ 417
现货
10 mg
¥ 777
现货
25 mg
¥ 1,297
现货
50 mg
¥ 1,948
现货
100 mg
¥ 2,923
现货
1 mL x 10 mM (in DMSO)
¥ 467
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产品介绍


Chelerythrine AI Summary
Chelerythrine exhibits a broad spectrum of bioactivities across diverse biochemical pathways and functions. It acts as an agonist for the NFkB Signaling Pathway (potency of 11220.2 nM) and the Thyroid Stimulating Hormone Receptor (potency of 25118.9 nM), as well as a potent inhibitor of various targets including HSD17B4 (25118.9 nM), Tyrosyl-DNA Phosphodiesterase (TDP1) (63095.7 nM), human liver OATP2B1 (13.1% inhibition), and recombinant human DOPA decarboxylase enzyme (IC50 of 1280000.0 nM). It inhibits mitochondrial division or activates mitochondrial fusion (5804.8 nM) and enhances SMN2 Splice Variant Expression (7079.5 nM). Notably, Chelerythrine shows strong binding affinity to c-myc and c-Kit1 G-quadruplex DNA, demonstrating significant antiproliferative activity against several human cancer cell lines, with complete inhibition of viability at 20 uM concentration in MTT assays. Additionally, Chelerythrine has pronounced antibacterial properties, effective against methicillin-resistant and methicillin-sensitive Staphylococcus aureus (MIC90 of 4.0 ug/mL), as well as vancomycin-resistant and vancomycin-sensitive Enterococcus faecalis (MIC90 of 32.0 ug/mL). It also inhibits Mycobacterium tuberculosis (MIC of 3.1 ug/mL). The compound displays competitive inhibition of human MAO-A (Ki of 220.0 nM) and MAO-B, favoring MAO-A with higher potency. It intervenes in cholinesterase activity, with IC50 values of 1450.0 nM for acetylcholinesterase (AChE) and 8580.0 nM for butyrylcholinesterase (BuChE), showing selectivity towards AChE. Chelerythrine also demonstrates selective cytotoxicity across different cell lines, with the highest potency against LL24 cells and the least against A549 cells. It furthers its bioactivity by binding to the PPARgamma ligand-binding domain (IC50 of 566.0 nM) and inhibiting SERCA1a activity with varied potencies (1200.0 nM to 27000.0 nM). These diverse activities suggest that Chelerythrine may have potential therapeutic applications in cancer, bacterial infections, neurodegenerative diseases, and metabolic disorders..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
1. Chelerythrine (Broussonpapyrine) may have antimanic effect . 2. Chelerythrine can inhibit telomerase activity. 3. Chelerythrine is a well-known protein kinase C inhibitor . 4. Chelerythrine has potential antiproliferative and antitumor effects.
靶点活性
PKC:0.7 μM (IC50)
别名白屈菜红碱, Toddalin, Cheleritrine, Broussonpapyrine
化学信息
分子量348.37
分子式C21H18NO4
CAS No.34316-15-9
SmilesC[N+]=1C=2C(C=3C(C1)=C(OC)C(OC)=CC3)=CC=C4C2C=C5C(=C4)OCO5
密度1.2985 g/cm3 (Estimated)
颜色Yellow
物理性状Solid
储存&溶解度
存储keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 11 mg/mL (31.58 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.8705 mL14.3526 mL28.7051 mL143.5256 mL
5 mM0.5741 mL2.8705 mL5.7410 mL28.7051 mL
10 mM0.2871 mL1.4353 mL2.8705 mL14.3526 mL
20 mM0.1435 mL0.7176 mL1.4353 mL7.1763 mL

TCMIP相关数据

中药材来源及性味归经
中药材名称中药材拉丁名归经
两面针Zanthoxylum nitidum (Roxb.) DC.苦, 辛肝, 胃
所属中成药
中成药名称处方组成中成药类型
宫炎平滴丸地稔,两面针,当归,五指毛桃,穿破石清热药
金花跌打酊红花,龙血竭,香附,两面针,樟脑,千斤拔,木香,白木香,乳香,没药,莪术,牛膝,骨碎补,金不换,黄柏,黄连,三叉苦木,鸭脚木皮,榕树须,土鳖虫活血化瘀药
鼻咽清毒剂野菊花,苍耳子,重楼,蛇泡簕,两面针,夏枯草,龙胆,党参清热药
复方风湿宁片两面针,七叶莲,宽筋藤,过岗龙,威灵仙,鸡骨香治风药
复方风湿宁注射液两面针,七叶莲,宽筋藤,过岗龙,威灵仙,鸡骨香祛风活络药
金鸡分散片金樱根,鸡血藤,千斤拔,功劳木,两面针,穿心莲清热药
复方风湿宁颗粒两面针,七叶莲,宽筋藤,过岗龙,威灵仙,鸡骨香治风药
复方风湿宁胶囊两面针,七叶莲,宽筋藤,过岗龙,威灵仙,鸡骨香治风药
活络止痛丸鸡血藤,何首乌,过岗龙,牛大力,莶草,豆豉姜,半枫荷,两面针,臭屎茉莉,走马胎,威灵,连钱草,千斤拔,独活,穿破石,薏苡仁,土五加,钩藤,山白芷,宽筋藤祛瘀药
华佗风痛宝胶囊红鱼眼,九层风,三叶青藤,山风(或大风艾),两面针,三七茎叶治风药
妇炎净片苦玄参,地胆草,当归,鸡血藤,两面针,横经席,柿叶,菥蓂,五指毛桃清热药
复方两面针漱齿液厚朴,两面针,薄荷脑清热药
妇炎净胶囊苦玄参,地胆草,当归,鸡血藤,两面针,横经席,柿叶,菥蓂,五指毛桃清热药
宫炎平分散片地稔,两面针,当归,五指毛桃,穿破石清热药
复方两面针含片西青果,两面针,山豆根,薄荷清热药
古威活络酊细辛,徐长卿,七味莲,两面针,古羊藤,十八症,鸡骨香,搜山虎,救必,应,九龙藤,大血藤,山花椒,良姜,威灵仙,千斤拔,桂枝,白芷,五加皮,防已,木香,泽兰,土鳖虫,续断,独活,薄荷脑,樟脑祛风活络药
金鸡丸金樱根,鸡血藤,千斤拨,功劳木,两面针,穿心莲清热药
宫炎平胶囊地稔,五指毛桃,两面针,穿破石,当归清热药
复方草玉梅含片草玉梅,两面针,射干,百合,地黄,玄参,岗梅,甘草,薄荷脑,薄荷素油,磷酸氢钙,香兰素清热药
蟾乌凝胶膏蟾酥,生川乌,两面针,重楼,生关白附,芙蓉叶,三棱,莪术,红花,丁香,细辛,肉桂,六轴子,荜菝,甘松,山奈,乳香,没药,薄荷脑,冰片,樟脑祛瘀药

计算器

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  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments 比如您的给药剂量是10 mg/kg,每只动物体重20g,给药体积100 μLTargetMol | Animal experiments 一共给药动物10只,您使用的配方为5%TargetMol | reagent DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline/PBS/ddH2O, 那么您的工作液浓度为2mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween80, 混匀澄清,再加 600μLSaline/PBS/ddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如: DMSOPEG300 / PEG400Tween 80SBE-β-CD玉米油 等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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