基本描述

别名	南蛇藤素
英文别名	(2R,4aS,6aR,6aS,14aS,14bR)-10-hydroxy-2,4a,6a,6a,9,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxylicacid \| IDI1_000718 \| MLS002701906 \| US9694016, 1156 \| NCGC00178913-14 \| Spectrum4_001966 \| BSPBio_001905 \| KBio2_003383 \| CHEBI:63959
规格或纯度	Moligand™, 分析标准品, ≥98%
英文名称	Celastrol
生化机理	Celastrol (Tripterin) 是一种源自植物的三萜类化合物。Celastrol(Tripterin) 具有抗炎和免疫抑制活性。Celastrol(Tripterin) 是一种抗氧化剂和抗炎剂。能有效抑制线粒体中的脂质过氧化反应，抑制 TNF-α 诱导的 NFκB 激活。体外实验也证明它能抑制拓扑异构酶 II 的活性（IC50 = 7.41 μM）。
应用	雷公藤红素是一种强力抗氧化，抗发炎剂。它是一种新型的HSP90的抑制剂（扰乱Hsp90/Cdc37复合物），抗癌（抗血管生成 - 抑制VEGFR的表达）;抗氧化剂（抑制脂质过氧化反应）和抗发炎活性（抑制iNOS及炎性细胞因子的生产）。
储存温度	-20°C储存
运输条件	超低温冰袋运输
作用类型	抑制剂
作用机制	G 蛋白信号调节抑制剂 17
产品介绍	存在于卫矛科植物雷公藤、南蛇藤等中的抗癌活性成分。该化合物结构载于2006年5月份Cancer Research杂志封面，并证实南蛇藤素通过抑制蛋白酶体活性进而诱发癌细胞凋亡，是有效的蛋白酶体抑制剂，其显著抑制了裸鼠身上前列腺癌的增生。因此，在癌症的预防和治疗方面，南蛇藤素是具有巨大开发潜力的天然蛋白酶体抑制剂。雷公藤红素是一种强力抗氧化，抗发炎剂。它是一种新型的HSP90的抑制剂（扰乱Hsp90/Cdc37复合物），抗癌（抗血管生成 - 抑制VEGFR的表达）;抗氧化剂（抑制脂质过氧化反应）和抗发炎活性（抑制iNOS及炎性细胞因子的生产）。 Celastrol, Celastrus scandens, a compound originally purified from Tripterygium wilfordii, has been shown to be an anti-peroxidative and anti-angiogenic agent. Mechanistic studies suggest that Celastrol suppresses levels of VEGF and Flk-1 receptors, VEGFR-1 and VEGFR-2, which may reduce signal transduction between the two growth factors. Additionally, Celastrol has demonstrated the ability to disrupt critical interaction of Glu33 (Hsp90) and Arg167 (Cdc37) in the superchaperone complex which causes anti-proliferative activity in vitro and inhibit Topo II (topoisomerase II) activity in vitro (IC50 = 7.41 μM). Celastrol, Celastrus scandens is an inhibitor of Hsp90.
纯度	≥98%

关联靶点（人）

HIF1A Tchem 缺氧诱导因子1-α(Hypoxia-inducible factor 1-alpha) (1 活性数据)

点击查看靶蛋白信息： HIF1A

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

TERT Tchem 端粒酶逆转录(Telomerase reverse transcriptase) (1 活性数据)

点击查看靶蛋白信息： TERT

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

RGS17 Tchem G 蛋白信号调节剂 17(Regulator of G-protein signaling 17) (0 活性数据)

点击查看靶蛋白信息： RGS17

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

名称和识别符

EC号	636-472-5
分子类型	小分子
IIUPAC Name	(2R,4aS,6aR,6aS,14aS,14bR)-10-hydroxy-2,4a,6a,6a,9,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxylic acid
INCHI	1S/C29H38O4/c1-17-18-7-8-21-27(4,19(18)15-20(30)23(17)31)12-14-29(6)22-16-26(3,24(32)33)10-9-25(22,2)11-13-28(21,29)5/h7-8,15,22,31H,9-14,16H2,1-6H3,(H,32,33)/t22-,25-,26-,27+,28-,29+/m1/s1
InChi Key	KQJSQWZMSAGSHN-JJWQIEBTSA-N
Smiles	CC1=C(C(=O)C=C2C1=CC=C3C2(CCC4(C3(CCC5(C4CC(CC5)(C)C(=O)O)C)C)C)C)O
Isomeric SMILES	CC1=C(C(=O)C=C2C1=CC=C3[C@]2(CC[C@@]4([C@@]3(CC[C@@]5([C@H]4C[C@](CC5)(C)C(=O)O)C)C)C)C)O
关联CAS	34157-83-0
NSC Number	70931
UN Number	2811
MeSH Entry Terms	3-hydroxy-24-nor-2-oxo-1(10),3,5,7-friedelatetraen-29-oic acid;celastrol;tripterin;tripterine
分子量	450.61
Reaxy-Rn	5780870
Reaxys-RN link address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=5780870&ln=

化学和物理性质

溶解性	Soluble in DMSO (>10 mg/ml), ethanol, DMF:PBS(pH 7.2)(1:10), and DMF. Insoluble in water.
密度	1.2
比旋光度	-122.7° (C=0.1,CHCl3)
熔点	203°C(lit.)
分子量	450.600 g/mol
XLogP3	5.900
氢键供体数Hydrogen Bond Donor Count	2
氢键受体数Hydrogen Bond Acceptor Count	4
可旋转键计数Rotatable Bond Count	1
精确质量Exact Mass	450.277 Da
单同位素质量Monoisotopic Mass	450.277 Da
拓扑极表面积Topological Polar Surface Area	74.600 Å²
重原子数Heavy Atom Count	33
形式电荷Formal Charge	0
复杂度Complexity	1100.000
同位素原子数Isotope Atom Count	0
定义的原子立体中心计数Defined Atom Stereocenter Count	6
未定义的原子立体中心计数Undefined Atom Stereocenter Count	0
定义的键立体中心计数Defined Bond Stereocenter Count	0
未定义的键立体中心计数Undefined Bond Stereocenter Count	0
所有立体化学键的总数The total count of all stereochemical bonds	0
共价键合单元计数Covalently-Bonded Unit Count	1

安全和危险性（GHS）

象形图	GHS06
信号词	危险
危险声明	H301: 吞咽会中毒
预防措施声明	P264: 处理后要彻底洗手。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P321: 特殊处理（请参阅此标签上的...）。 P330: 漱口 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P301+P316: 如果吞咽：立即寻求紧急医疗救助。
WGK Germany	2
个人防护装备	Eyeshields,Faceshields,Gloves,type P2 (EN 143) respirator cartridges

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找到6个结果

批号(Lot Number)	证书类型	货号
F2518326	分析证书	C107671
A2517305	分析证书	C107671
A2517308	分析证书	C107671
I2116200	分析证书	C107671
C2218431	分析证书	C107671
C2218450	分析证书	C107671

此产品的引用文献

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引用文献

1. Allison AC, Cacabelos R, Lombardi VR, Alvarez XA, Vigo C. (2001) Celastrol, a potent antioxidant and anti-inflammatory drug, as a possible treatment for Alzheimer's disease.. Prog Neuropsychopharmacol Biol Psychiatry, 25 (7): (1341-57). [PMID:11513350]
2. Pfuhlmann K, Schriever SC, Baumann P, Kabra DG, Harrison L, Mazibuko-Mbeje SE, Contreras RE, Kyriakou E, Simonds SE, Tiganis T et al.. (2018) Celastrol-Induced Weight Loss Is Driven by Hypophagia and Independent From UCP1.. Diabetes, 67 (11): (2456-2465). [PMID:30158241]
3. Zhan X, Yan C, Chen Y, Wei X, Xiao J, Deng L, Yang Y, Qiu P, Chen Q. (2018) Celastrol antagonizes high glucose-evoked podocyte injury, inflammation and insulin resistance by restoring the HO-1-mediated autophagy pathway.. Mol Immunol, 104 (61-68). [PMID:30439604]
4. Wong VKW, Qiu C, Xu SW, Law BYK, Zeng W, Wang H, Michelangeli F, Dias IRSR, Qu YQ, Chan TW et al.. (2019) Ca²⁺ signalling plays a role in celastrol-mediated suppression of synovial fibroblasts of rheumatoid arthritis patients and experimental arthritis in rats.. Br J Pharmacol, 176 (16): (2922-2944). [PMID:31124139]
5. Shi K, Chen X, Xie B, Yang SS, Liu D, Dai G, Chen Q. (2018) Celastrol Alleviates Chronic Obstructive Pulmonary Disease by Inhibiting Cellular Inflammation Induced by Cigarette Smoke via the Ednrb/Kng1 Signaling Pathway.. Front Pharmacol, 9 (1276). [PMID:30498444]
6. Zhang J, Zhou K, Zhang X, Zhou Y, Li Z, Shang F. (2019) Celastrol Ameliorates Inflammation in Human Retinal Pigment Epithelial Cells by Suppressing NF-κB Signaling.. J Ocul Pharmacol Ther, 35 (2): (116-123). [PMID:30596540]
7. Zhou X, Cao X, Tu H, Zhang ZR, Deng L. (2019) Inflammation-Targeted Delivery of Celastrol via Neutrophil Membrane-Coated Nanoparticles in the Management of Acute Pancreatitis.. Mol Pharm, 16 (3): (1397-1405). [PMID:30753778]
8. Venkatesha SH, Moudgil KD. (2019) Celastrol suppresses experimental autoimmune encephalomyelitis via MAPK/SGK1-regulated mediators of autoimmune pathology.. Inflamm Res, 68 (4): (285-296). [PMID:30820608]
9. Feng X, Guan D, Auen T, Choi JW, Salazar Hernández MA, Lee J, Chun H, Faruk F, Kaplun E, Herbert Z et al.. (2019) IL1R1 is required for celastrol's leptin-sensitization and antiobesity effects.. Nat Med, 25 (4): (575-582). [PMID:30833749]
10. Ping Sheng, Chao Bu, Tanyue Hui, Lili Zhou, Hao Chen, Guoliang Zhou. (2023) Polydopamine-activated celastrol carbon dots for synergistic chemotherapy-photothermal therapy of tumors. International Journal of Pharmaceutics-X, 6 (100218). [PMID:38033396] [10.1016/j.ijpx.2023.100218]
11. Jiwen Fan, Meng Ren, Weiwei Chen, Haodong Wang, Yuquan He. (2023) Celastrol relieves myocardial infarction-induced cardiac fibrosis by inhibiting NLRP3 inflammasomes in rats. INTERNATIONAL IMMUNOPHARMACOLOGY, 121 (110511). [PMID:37343368] [10.1016/j.intimp.2023.110511]
12. Xiaoli Li, Guangbei Zhu, Xintong Yao, Ning Wang, Ronghui Hu, Qingxin Kong, Duanfang Zhou, Liangyuan Long, Jiali Cai, Weiying Zhou. (2022) Celastrol induces ubiquitin-dependent degradation of mTOR in breast cancer cells. OncoTargets and Therapy, [PMID:30588010] [10.2147/OTT.S187315]
13. Qiang Chen, Chunjing Guo, Zhongxin Liu, Min Cao, Wenxin Wang, Dandan Zhang, Hongxu Geng, Ningning Diao, Daquan Chen. (2023) Multifunctional nanoparticles with anti-inflammatory effect for improving metabolic syndromes. JOURNAL OF DRUG TARGETING, 31 (3): (286-295). [PMID:36315421] [10.1080/1061186X.2022.2142595]
14. Bo Yu, Yiping Shen, Xuejie Zhang, Lijuan Ding, Zheng Meng, Xiaotong Wang, Meihua Han, Yifei Guo, Xiangtao Wang. (2022) Poly(methacrylate citric acid) as a Dual Functional Carrier for Tumor Therapy. Pharmaceutics, 14 (9): (1765). [PMID:36145512] [10.3390/pharmaceutics14091765]
15. Lin Jingpan, Gao Lu, Lin Yanke, Wang Shuai, Yang Zemin, Ren Shujing, Chen Min, Wu Baojian. (2021) Pharmacokinetics-Based Chronoefficacy of Semen Strychni and Tripterygium Glycoside Tablet Against Rheumatoid Arthritis. Frontiers in Pharmacology, 12 [PMID:34108880] [10.3389/fphar.2021.673263]
16. Niu Weina, Wang Jianguo, Wang Qinyao, Shen Jianjun. (2020) Celastrol Loaded Nanoparticles With ROS-Response and ROS-Inducer for the Treatment of Ovarian Cancer. Frontiers in Chemistry, 8 [PMID:33195064] [10.3389/fchem.2020.574614]
17. Zhao Huan, Tong Yongbin, Lu Danyi, Wu Baojian. (2020) Circadian clock regulates hepatotoxicity of Tripterygium wilfordii through modulation of metabolism. JOURNAL OF PHARMACY AND PHARMACOLOGY, 72 (12): (1854-1864). [PMID:32478421] [10.1111/jphp.13299]
18. Jian Lu, Daozhi Liu, Xiaojing Zhou, Ang Chen, Zhenran Jiang, Xiyun Ye, Mingyao Liu, Xin Wang. (2018) Plant natural product plumbagin presents potent inhibitory effect on human cytochrome P450 2J2 enzyme. PHYTOMEDICINE, 39 (137). [PMID:29433675] [10.1016/j.phymed.2017.12.026]
19. Yang Hongbin, Liu Chang, Jiang Jie, Wang Yuena, Zhang Xiaoyu. (2017) Celastrol Attenuates Multiple Sclerosis and Optic Neuritis in an Experimental Autoimmune Encephalomyelitis Model. Frontiers in Pharmacology, 8 [PMID:28239352] [10.3389/fphar.2017.00044]
20. Yunpeng Qi,Renping Wang,Liang Zhao,Lei Lv,Fan Zhou,Tian Zhang,Feng Lu,Hongli Yan,Gengli Duan. (2018-08-03) Celastrol Suppresses Tryptophan Catabolism in Human Colon Cancer Cells as Revealed by Metabolic Profiling and Targeted Metabolite Analysis.. Biological & pharmaceutical bulletin, 41 ((8)): (1243-1250). [PMID:30068874]
21. Hu Yingying, Nan Yan, Lin Hongzhou, Zhao Qianlei, Chen Tingting, Tao Xiaoyue, Ding Bingqing, Lu Liying, Chen Shangqin, Zhu Jianghu, Guo Xiaoling, Lin Zhenlang. (2024) Celastrol ameliorates hypoxic-ischemic brain injury in neonatal rats by reducing oxidative stress and inflammation. PEDIATRIC RESEARCH, (1-12). [PMID:38763946] [10.1038/s41390-024-03246-9]
22. Yunyan Chen, Ziwei Zhang, Zhilei Qian, Rui Ma, Minna Luan, Yu Sun. (2024) Sequentially Released Liposomes Enhance Anti-Liver Cancer Efficacy of Tetrandrine and Celastrol-Loaded Coix Seed Oil. International Journal of Nanomedicine, [PMID:38288265] [10.2147/IJN.S446895]

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货号 (SKU)	包装规格	是否现货
C107671-10mg	10mg	现货
C107671-20mg	20mg	现货
C107671-50mg	50mg	现货

雷公藤红素, G 蛋白信号调节抑制剂 17

库存信息

库存信息

库存信息

基本描述

关联靶点（人）

名称和识别符

化学和物理性质

安全和危险性（GHS）

质检证书（CoA,COO,BSE/TSE 和分析图谱)

此产品的引用文献

引用文献

溶液计算器

摩尔浓度计算器

稀释计算器

复溶计算器