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雷公藤甲素

抑制RNAPII介导的转录;抗肿瘤,抗炎和免疫抑制
    级别和纯度:
  • ≥98%
有货

库存信息

关闭
货号 (SKU) 包装规格 是否现货 价格 数量
T107400-50mg
50mg 期货 Stock Image

基本描述

别名 雷公藤甲素
英文别名 PG 490 | HY-32735 | NSC839303 | NSC-839303 | CAS-5611-51-8 | SCHEMBL413634 | MLS000759410 | NCGC00163411-02 | BSPBio_001595 | Triptolid | NCGC00163411-01 | (5bS,6aS,7aS,8R,8aR,9aS,9bS,10aS,10bS)-8-Hydroxy-8a-isopropyl-10b-methyl-1,5,5b,6,6a,8,8a,9a,9b,10b
规格或纯度 ≥98%
英文名称 Triptolide
生化机理 抑制XBP的DNA依赖性ATPase活性并诱导抑制RNA聚合酶II(RNAPII)介导的转录(IC50 = 200 nM)。相对于RNAPI和RNAPIII具有选择性。阻止HeLa细胞中的RNA合成(IC50 = 62 nM);在60个癌细胞系中表现出有效的抗增殖活性(平均IC50 = 12 nM),并通过阻断TNF-α介导的c-IAP1和c-IAP2诱导细胞凋亡。还显示出免疫抑制和抗炎活性。
储存温度 2-8°C储存
运输条件 冰袋运输
产品介绍

雷公藤甲素是一个具有多种生物活性的二萜内酯,可溶于二甲基亚砜.来源于中药雷公藤的根

纯度 ≥98%

关联靶点(人)

F2RL1 Tchem 蛋白酶激活受体 2(Proteinase-activated receptor 2) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
PTGS2 Tclin 前列腺素 G/H 合酶 2(Prostaglandin G/H synthase 2) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
AR Tclin Androgen Receptor (11781 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PTGS2 Tclin Cyclooxygenase-2 (13999 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
A498 (42825 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ACHN (49357 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BGC-823 (3035 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CAKI-1 (44928 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CCRF-CEM (65223 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CFPAC-1 (421 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
COLO 205 (50209 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DU-145 (51482 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HL-60 (67320 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HT-29 (80576 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
K562 (73714 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KM12 (47707 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
M14 (47487 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MCF7 (126967 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MDA-MB-468 (9477 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NCI-H1975 (4994 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MKN-28 (466 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MOLT-4 (49676 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OVCAR-3 (48710 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OVCAR-4 (44535 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OVCAR-5 (45555 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OVCAR-8 (47708 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PANC-1 (6144 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PC-3 (62116 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPMI-8226 (44974 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RXF 393 (41971 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SF-295 (48000 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SGC-7901 (2773 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SK-MEL-2 (46422 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SK-MEL-28 (48833 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SK-MEL-5 (47095 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SK-OV-3 (52876 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SN12C (47755 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SNB-19 (46794 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SW480 (6023 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TK-10 (45540 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
U-251 (51189 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
UACC-257 (46019 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
UACC-62 (47335 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
UO-31 (46270 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
786-0 (47912 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
A549 (127892 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Bel-7402 (4577 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BJ (6930 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NCI/ADR-RES (33767 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
T47D (39041 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MIA PaCa-2 (5949 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EKVX (44102 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点(其它种属)

Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Pseudomonas aeruginosa (123386 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Klebsiella pneumoniae (43867 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Staphylococcus aureus (210822 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Acinetobacter baumannii (41033 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Escherichia coli (133304 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cryptococcus neoformans (21258 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Candida albicans (78123 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Caenorhabditis elegans (1055 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CV-1 (316 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MDCK (10148 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MEF (1005 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RAW264.7 (28094 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NIH3T3 (5395 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hsf1 Heat shock factor protein 1 (5445 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rorc Nuclear receptor ROR-gamma (89407 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ffp 4'-phosphopantetheinyl transferase ffp (24982 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

PubChem SID 504756646
分子类型 小分子
IIUPAC Name (1S,2S,4S,5S,7R,8R,9S,11S,13S)-8-hydroxy-1-methyl-7-propan-2-yl-3,6,10,16-tetraoxaheptacyclo[11.7.0.02,4.02,9.05,7.09,11.014,18]icos-14(18)-en-17-one
INCHI 1S/C20H24O6/c1-8(2)18-13(25-18)14-20(26-14)17(3)5-4-9-10(7-23-15(9)21)11(17)6-12-19(20,24-12)16(18)22/h8,11-14,16,22H,4-7H2,1-3H3/t11-,12-,13-,14-,16+,17-,18-,19+,20+/m0/s1
InChi Key DFBIRQPKNDILPW-CIVMWXNOSA-N
Smiles CC(C)C12C(O1)C3C4(O3)C5(CCC6=C(C5CC7C4(C2O)O7)COC6=O)C
Isomeric SMILES CC(C)[C@@]12[C@@H](O1)[C@H]3[C@@]4(O3)[C@]5(CCC6=C([C@@H]5C[C@H]7[C@]4([C@@H]2O)O7)COC6=O)C
PubChem CID 107985
分子量 360.4
Reaxy-Rn 1692435

化学和物理性质

溶解性 溶于DMSO, 最高浓度 (mg/mL): 7.21, 最高浓度(mM): 20
密度 1.48
敏感性 对热敏感
熔点 229 °C
分子量 360.400 g/mol
XLogP3 0.200
氢键供体数Hydrogen Bond Donor Count 1
氢键受体数Hydrogen Bond Acceptor Count 6
可旋转键计数Rotatable Bond Count 1
精确质量Exact Mass 360.157 Da
单同位素质量Monoisotopic Mass 360.157 Da
拓扑极表面积Topological Polar Surface Area 84.100 Ų
重原子数Heavy Atom Count 26
形式电荷Formal Charge 0
复杂度Complexity 819.000
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 9
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,   GHS08
信号词 Danger
WGK Germany 3
RTECS YK7751000
Merck Index 9747
个人防护装备 Eyeshields,Gloves,type N95 (US),type P1 (EN143) respirator filter

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批号(Lot Number) 证书类型 货号
H2302761 分析证书 T107400
D2304109 分析证书 T107400
D2304114 分析证书 T107400
D2304112 分析证书 T107400

此产品的引用文献

引用文献

1. 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]
2. 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]
3. Lin Yanke, Wang Shuai, Zhou Ziyue, Guo Lianxia, Yu Fangjun, Wu Baojian.  (2019)  Bmal1 regulates circadian expression of cytochrome P450 3a11 and drug metabolism in mice.  Communications Biology,  (1): (1-11).  [PMID:31633069] [10.1038/s42003-019-0607-z]
4. Caili Huang, Tao Zeng, Jiawen Li, Lishan Tan, Xiulong Deng, Yanchao Pan, Qi Chen, Aiqing Li, Jianqiang Hu.  (2019)  Folate Receptor-Mediated Renal-Targeting Nanoplatform for the Specific Delivery of Triptolide to Treat Renal Ischemia/Reperfusion Injury.  ACS Biomaterials Science & Engineering,  (6): (2877–2886).  [PMID:33405591] [10.1021/acsbiomaterials.9b00119]
5. Bailing Ma, Mi Lu, Bo-Yang Yu, Jiangwei Tian.  (2018)  A galactose-mediated targeting nanoprobe for intracellular hydroxyl radical imaging to predict drug-induced liver injury.  RSC Advances,  (39): (22062-22068).  [PMID:35541760] [10.1039/C8RA01424H]
6. Yanrong Zhu, Lichen Yao, Yilei Guo, Jing Zhang, Yufeng Xia, Zhifeng Wei, Yue Dai.  (2024)  Bergenin attenuates triptolide-caused premature ovarian failure in mice based on the antioxidant activity.  REPRODUCTIVE TOXICOLOGY,  (108608).  [PMID:38735593] [10.1016/j.reprotox.2024.108608]
7. Huahui Zeng, Man Li, Zhirong Wang, Tianqi Wang, Zhenqiang Zhang, Xiangxiang Wu.  (2024)  Disulfide bond-based oxidation-responsive triptolide-loaded nanodrug for inflammation-targeted treatment of collagen-induced arthritis.  Applied Materials Today,  40  (102350).  [10.1016/j.apmt.2024.102350]
8. Meizhen Yin, Xinying Zhang, Tongguang Zhang, Zhiqiang Bao, Zhihui He.  (2024)  Folic Acid-Targeted Mixed Pluronic Micelles for Delivery of Triptolide.  Polymers,  16  (24): (3485).  [PMID:39771337] [10.3390/polym16243485]
9. Abudureheman Bahatibieke, Jianming Zhao, Danping Fan, Zixiang Zhou, Junfei Li, Xing Wang, Hongyan Zhao, Tianyang Wang, Ziyuan Fang, Yajie Xie, Cheng Huang, Cheng Xiao, Yudong Zheng.  (2025)  Sea-Island Micelle Structured Hydrogel Scaffold: A Dual-Action Approach to Combat Cartilage Damage under RA Conditions.  ACS Applied Materials & Interfaces,  [PMID:39746184] [10.1021/acsami.4c16005]

溶液计算器