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川皮苷, TAS2R14 的激动剂

聚甲氧基黄酮。强大的MMP抑制剂。
6篇引用文献 COA COA
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货号 (SKU) 包装规格 是否现货 价格 数量
N130078-50mg
 50mg 现货 Stock Image
N130078-250mg
 250mg 现货 Stock Image
N130078-1g
 1g 现货 Stock Image
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Apoptosis (7108) Autophagy (2848) Glucose Metabolism (3713) Immunology/Inflammation (1938) Metabolic Enzyme/Protease (4889) NF-κB (756) Reactive Oxygen Species (316) ROR (47) TAS2R14 Agonist (20) Vitamin D Related/Nuclear Receptor (908) 脂质代谢 (4331)
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基本描述

别名 蜜橘黄素 | 川陈皮素 | 3',4',5,6,7,8-六甲氧基黄酮 | 川皮亭 | 2-（3,4-二羟基苯基）-5,6,7,8-三羟基-4 H -1-苯并吡喃-4-酮
英文别名 SPBio_001654 | NC00186 | Spectrum3_000921 | 2-(3,4-Dimethoxyphenyl)-5,6,7,8-tetramethoxy-4H-1-benzopyran-4-one | GTPL12446 | HMS2234A09 | MFCD03273560 | AKOS015965334 | FT-0686667 | MLS000759462 | NSC76751 | 2-(3,4-dimethoxyphenyl)-5,6,7,8-tetramethoxy-4H
规格或纯度 Moligand™, ≥95%(HPLC)
英文名称 Nobiletin
生化机理 金莲花素能抑制基质金属蛋白酶 1、3 和 9 的表达，这些酶在肿瘤转移过程中参与细胞外基质的分解。金没药素还能增加基质金属蛋白酶 1 组织抑制剂的表达，进一步阻止肿瘤侵袭过程中细胞外基质的降解。这种生物类黄酮被认为是通过破坏 Ras-Raf-MEK 信号转导途径来实现上述两种功能的。强效 MMP 抑制剂。抑制促 MMP-1、3 和 9 的产生。在体内具有抗炎和抗肿瘤作用。具有口服活性。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 激动剂
作用机制 TAS2R14 的激动剂
备注 如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍

Nobiletin is a flavanoid with antioxidant and anti-inflammatory properties found in the rind of tangerines. The compound has been observed to inhibit the phosphorylation of MEK (mitogen-activated protein kinase). Nobiletin has also been documented to suppress the expression of MMP-1 (matrix metalloproteinases), MMP-3 and MMP-9 that are involved in the breakdown of the extracellular matrix during tumor metastasis. In vitro studies of Nobiletin on varying cancer cell lines and on the chick egg has shown the anti-angiogenic effects of Nobiletin throμgh down regulation of ERK 1, ERK 2 and c-Jun N-terminal kinase, and transcriptional factors c-Jun and Stat3. The compound also suppressed proliferation, migration and tube formation on matrigel of HUVEC cells stimulated with growth supplement. Nobiletin has demonstrated to attenuate NF-κB transcriptional activation, NO and PGE2 production, NOS2 (inducible nitric oxide synthase) and Cox-2 (cyclooxygenase-2) expression.An antioxidant and anti-inflammatory that Inhibits the phosphorylation of MEK.

Nobiletin is a flavanoid with antioxidant and anti-inflammatory properties found in the rind of tangerines. The compound has been observed to inhibit the phosphorylation of MEK (mitogen-activated protein kinase). Nobiletin has also been documented to suppress the expression of MMP-1 (matrix metalloproteinases), MMP-3 and MMP-9 that are involved in the breakdown of the extracellular matrix during tumor metastasis. In vitro studies of Nobiletin on varying cancer cell lines and on the chick egg has shown the anti-angiogenic effects of Nobiletin through down regulation of ERK 1, ERK 2 and c-Jun N-terminal kinase, and transcriptional factors c-Jun and Stat3. The compound also suppressed proliferation, migration and tube formation on matrigel of HUVEC cells stimulated with growth supplement. Nobiletin has demonstrated to attenuate NF-κB transcriptional activation, NO and PGE2 production, NOS2 (inducible nitric oxide synthase) and Cox-2 (cyclooxygenase-2) expression.
An antioxidant and anti-inflammatory that Inhibits the phosphorylation of MEK.
纯度 ≥95%(HPLC)

关联靶点（人）

TAS2R14 Tchem 2 型味觉受体成员 14(Taste receptor type 2 member 14) (0 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)
PPARG Tclin Peroxisome proliferator-activated receptor gamma (15191 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
XDH Tclin Xanthine dehydrogenase (1038 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
APP Tclin Amyloid-beta A4 protein (8510 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ALDH1A1 Tchem Aldehyde dehydrogenase 1A1 (77053 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GLP1R Tclin Glucagon-like peptide 1 receptor (111429 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PIN1 Tchem Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (36611 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 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
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
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
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
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
Panel NCI-60 (60 carcinoma cell lines) (1088 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
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
SH-SY5Y (11521 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
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
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
EKVX (44102 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NCI-H322M (45589 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HCC 2998 (41480 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HCT-116 (91556 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HOP-92 (41141 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hs-578T (29457 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）

ampC Beta-lactamase AmpC (62480 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cruzipain (33337 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Abcb1b P-glycoprotein 1 (174 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
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
Salmonella typhimurium (15756 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
Aspergillus niger (16508 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Plasmodium falciparum (966862 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
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
3T3-L1 (3664 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PC-12 (7051 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
Lewis lung carcinoma cell line (1243 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GCN5 Histone acetyltransferase GCN5 (89 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
Phytophthora citrophthora (55 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Spodoptera litura (1708 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mapt Microtubule-associated protein tau (6 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
Citrus (8 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

分子类型 小分子
IIUPAC Name 2-(3,4-dimethoxyphenyl)-5,6,7,8-tetramethoxychromen-4-one
INCHI 1S/C21H22O8/c1-23-13-8-7-11(9-15(13)24-2)14-10-12(22)16-17(25-3)19(26-4)21(28-6)20(27-5)18(16)29-14/h7-10H,1-6H3
InChi Key MRIAQLRQZPPODS-UHFFFAOYSA-N
Smiles COC1=C(C=C(C=C1)C2=CC(=O)C3=C(O2)C(=C(C(=C3OC)OC)OC)OC)OC
Isomeric SMILES COC1=C(C=C(C=C1)C2=CC(=O)C3=C(O2)C(=C(C(=C3OC)OC)OC)OC)OC
关联CAS 478-01-3
NSC Number 76751
MeSH Entry Terms hexamethoxyflavone;nobiletin
分子量 402.39
Beilstein号 360887
Reaxy-Rn 360887
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=360887&ln=

化学和物理性质

溶解性 Soluble in methanol ( ), water (<1 mg/ml), chloroform, DMSO (81 mg/ml), and ethanol (3 mg/ml).
敏感性 对热敏感
熔点 138°C
分子量 402.400 g/mol
XLogP3 3.000
氢键供体数Hydrogen Bond Donor Count 0
氢键受体数Hydrogen Bond Acceptor Count 8
可旋转键计数Rotatable Bond Count 7
精确质量Exact Mass 402.131 Da
单同位素质量Monoisotopic Mass 402.131 Da
拓扑极表面积Topological Polar Surface Area 81.700 Ų
重原子数Heavy Atom Count 29
形式电荷Formal Charge 0
复杂度Complexity 593.000
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 0
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）

WGK Germany 3
RTECS DJ3052200

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批号(Lot Number) 证书类型 货号
G2523617 分析证书 N130078
G2523618 分析证书 N130078
G2523619 分析证书 N130078
G2523620 分析证书 N130078
G2523621 分析证书 N130078
C1702052 分析证书 N130078
I2017234 分析证书 N130078

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引用文献

1. Tingting Jin, Na Li, Yi Wu, Ying He, Depo Yang, Feng He.  (2023)  Nobiletin with AIEE Characteristics for Targeting Mitochondria and Real-Time Dynamic Tracking in Zebrafish.  MOLECULES,  28  (12): (4592).  [PMID:37375147] [10.3390/molecules28124592]
2. Min Chen, Yifei Xiao, Fugui Zhang, Jianhao Du, Li Zhang, Yifang Li, Danyi Lu, Zhigang Wang, Baojian Wu.  (2022)  Tangeretin prevents cognitive deficit in delirium through activating RORα/γ-E4BP4 axis in mice.  BIOCHEMICAL PHARMACOLOGY,  205  (115286).  [PMID:36216079] [10.1016/j.bcp.2022.115286]
3. Qi Quan, Wei Liu, Jiajing Guo, Meiling Ye, Juhua Zhang.  (2022)  Effect of Six Lactic Acid Bacteria Strains on Physicochemical Characteristics, Antioxidant Activities and Sensory Properties of Fermented Orange Juices.  Foods,  11  (13): (1920).  [PMID:35804736] [10.3390/foods11131920]
4. Xin Huang, Junxiang Zhu, Li Wang, Huijuan Jing, Chaoyang Ma, Xingran Kou, Hongxin Wang.  (2020)  Inhibitory mechanisms and interaction of tangeretin, 5-demethyltangeretin, nobiletin, and 5-demethylnobiletin from citrus peels on pancreatic lipase: Kinetics, spectroscopies, and molecular dynamics simulation.  INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES,  164  (1927).  [PMID:32795575] [10.1016/j.ijbiomac.2020.07.305]
5. Lili Guo, Huijun Zheng, Cuijie Zhang, Lingbo Qu, Lanlan Yu.  (2020)  A novel molecularly imprinted sensor based on PtCu bimetallic nanoparticle deposited on PSS functionalized graphene with peroxidase-like activity for selective determination of puerarin.  TALANTA,  210  (120621).  [PMID:31987162] [10.1016/j.talanta.2019.120621]
6. Xue Wang, Zhipeng Su, Xiang Li, Jiaxu Chen, Gaoyang Li, Yang Shan, Zhaoping Pan, Fuhua Fu.  (2024)  Targeted/untargeted metabolomics and antioxidant properties distinguish Citrus reticulata ‘Chachi’ from Citrus reticulata Blanco.  FOOD CHEMISTRY,  (140806).  [PMID:39241684] [10.1016/j.foodchem.2024.140806]

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