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咪喹莫特, TLR7 激动剂

Toll样受体7激动剂；免疫调节剂
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货号 (SKU) 包装规格 是否现货 价格 数量
I129798-50mg
 50mg 现货 Stock Image
I129798-100mg
 100mg 现货 Stock Image
I129798-250mg
 250mg 现货 Stock Image
I129798-500mg
 500mg 现货 Stock Image
I129798-1g
 1g 现货 Stock Image
I129798-5g
 5g 现货 Stock Image
I129798-25g
 25g 现货 Stock Image
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Anti-infection (2804) Autophagy (2848) HSV (103) Immunology/Inflammation (1938) SARS-CoV冠状病毒 (200) TLR7 Agonist (5) Toll-like Receptor (TLR) (149) Virus (3767)
main product photo

基本描述

别名 咪喹莫特 | 1-(2-甲基丙基)-1 H -咪唑 4,5- c 喹啉-4-胺 | 1-(2-甲基丙基)-4-氨基-1H-咪唑并[4,5-c]喹啉 | 1-异丁基-1H-咪唑[4.5-C]喹啉-4-胺基 | 4-氨基-1-异丁基-1H-咪唑并[4,5-c]喹啉
英文别名 HMS3715N19 | Imiquimod 100 microg/mL in Acetonitrile | Imiquimod- Bio-X | Aldara (TN) | DTXSID7041047 | HY-B0180 | S 26308 | AB00399298-05 | IMIQUIMOD [ORANGE BOOK] | YH44175 | 1-isobutylimidazo[4,5-c]quinolin-4-amine | HB3109 | IMIQUIMOD [JAN] | 4-Amino-
规格或纯度 Moligand™, ≥98%
英文名称 Imiquimod
生化机理 咪喹莫特是咪唑喹啉胺的衍生物，可抑制血管生成，是一种免疫反应调节剂。有研究报告称，咪喹莫特能够抑制转移和诱导α-干扰素（IFN-α）。此外，咪喹莫特还是一种TLR7（toll样受体7）激动剂，可诱导浆细胞树突状细胞（pDC）成熟。咪喹莫特作用于表达 TLR7 的树突状细胞，诱导免疫反应。核因子-B有助于介导咪喹莫特的活性，并参与提高趋化因子和细胞因子的水平。研究表明，Imiquimod 的抗血管生成特性是由 IL-18 介导的。研究表明，咪喹莫特能诱导癌细胞凋亡。还被证实是一种 Caspase-3 和 NFκB 的激活剂。激活 NF-κB，刺激促炎细胞因子。免疫调节剂、抗病毒剂和抗肿瘤剂。在体内和体外均有活性。
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 TLR7 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。有毒，请参阅SDS以获取更多信息。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


Product Description

Imiquimod (R 837) is an immune response modifier that acts as a toll-like receptor 7 agonist.
A TLR7 activator and angiogenesis inhibitor.

Product Application

Imiquimod is a caspase 3 activator which acts as an immunomodulator and displays antiviral and anti-tumor activity. It is a patient-applied cream used for the treatment of genital warts and basal cell carcinoma. It is also used to cure actinic keratosis on the face and scalp. It belongs to a group of drugs called immune response modifiers, which work by activating the immune system to fight abnormal skin growth.
纯度 ≥98%

关联靶点（人）

NUDT1 Tchem 7,8-二氢-8-氧鸟嘌呤三磷酸酶(7,8-dihydro-8-oxoguanine triphosphatase) (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)
TLR7 Tclin Toll 类受体 7(Toll-like receptor 7) (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)
PDE5A Tclin Phosphodiesterase 5A (5113 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CA2 Tclin Carbonic anhydrase II (17698 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ESR1 Tclin Estrogen receptor alpha (17718 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HMGCR Tclin HMG-CoA reductase (2475 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NR3C1 Tclin Glucocorticoid receptor (14987 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
INSR Tclin Insulin receptor (5558 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PGR Tclin Progesterone receptor (8562 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRB2 Tclin Beta-2 adrenergic receptor (11824 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRB1 Tclin Beta-1 adrenergic receptor (6630 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
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
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ACE Tclin Angiotensin-converting enzyme (1423 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD2 Tclin Dopamine D2 receptor (23596 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GABRA1 Tclin GABA receptor alpha-1 subunit (399 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAOA Tclin Monoamine oxidase A (11911 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CNR1 Tclin Cannabinoid CB1 receptor (20913 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD4 Tchem Dopamine D4 receptor (7907 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ACHE Tclin Acetylcholinesterase (18204 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PTGS1 Tclin Cyclooxygenase-1 (9233 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A2 Tclin Norepinephrine transporter (10102 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH2 Tclin Histamine H2 receptor (5428 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA1D Tclin Alpha-1d adrenergic receptor (4171 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR1B Tclin Serotonin 1b (5-HT1b) receptor (2801 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2A Tclin Serotonin 2a (5-HT2a) receptor (14758 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2C Tclin Serotonin 2c (5-HT2c) receptor (11471 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AVPR2 Tclin Vasopressin V2 receptor (2912 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADORA1 Tclin Adenosine A1 receptor (17603 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AGTR1 Tclin Type-1 angiotensin II receptor (5176 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CALCR Tclin Calcitonin receptor (2215 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A4 Tclin Serotonin transporter (12625 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA1A Tclin Alpha-1a adrenergic receptor (8359 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
HRH1 Tclin Histamine H1 receptor (7573 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA1B Tclin Alpha-1b adrenergic receptor (2912 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD3 Tclin Dopamine D3 receptor (14368 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AVPR1A Tclin Vasopressin V1a receptor (5412 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRD1 Tclin Delta opioid receptor (15096 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRK1 Tclin Kappa opioid receptor (16155 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR3A Tclin Serotonin 3a (5-HT3a) receptor (3366 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A3 Tclin Dopamine transporter (10535 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GRIN1 Tclin Glutamate (NMDA) receptor subunit zeta 1 (122 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KCNH2 Tclin HERG (29587 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR4 Tclin Serotonin 4 (5-HT4) receptor (2068 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CACNA1C Tclin Voltage-gated L-type calcium channel alpha-1C subunit (766 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）

Agtr2 Angiotensin II type 2 (AT-2) receptor (803 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mc4r Melanocortin receptor 4 (1205 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Ltc4s Leukotriene C4 synthase (1 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Sigmar1 Sigma opioid receptor (160 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Npy1r Neuropeptide Y receptor type 1 (8 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cckar Cholecystokinin A receptor (90 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Pde4d Phosphodiesterase 4D (4 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Nos2 Nitric oxide synthase, inducible (3573 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
Mmp9 Matrix metalloproteinase 9 (38 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
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
Hepatitis C virus (23859 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
Tlr7 Toll-like receptor 7 (174 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Tlr7 TLR7 and TLR8 (70 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Glra2 Glycine receptor (1745 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
TLR7 Toll-like receptor 7/8 (156 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 488183396
分子类型 小分子
IIUPAC Name 1-(2-methylpropyl)imidazo[4,5-c]quinolin-4-amine
INCHI 1S/C14H16N4/c1-9(2)7-18-8-16-12-13(18)10-5-3-4-6-11(10)17-14(12)15/h3-6,8-9H,7H2,1-2H3,(H2,15,17)
InChi Key DOUYETYNHWVLEO-UHFFFAOYSA-N
Smiles CC(C)CN1C=NC2=C1C3=CC=CC=C3N=C2N
Isomeric SMILES CC(C)CN1C=NC2=C1C3=CC=CC=C3N=C2N
分子量 240.31
Reaxy-Rn 7710060
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7710060&ln=

化学和物理性质

溶解性 Soluble in DMSO (4 mg/ml ,warming to 60 °C for 15 minutes) DMF (1.5 mg/ml) at 37 °C, and water (slightly soluble) at 37 °C. Insoluble in ethanol.
熔点 297~299℃
分子量 240.300 g/mol
XLogP3 2.600
氢键供体数Hydrogen Bond Donor Count 1
氢键受体数Hydrogen Bond Acceptor Count 3
可旋转键计数Rotatable Bond Count 2
精确质量Exact Mass 240.137 Da
单同位素质量Monoisotopic Mass 240.137 Da
拓扑极表面积Topological Polar Surface Area 56.700 Ų
重原子数Heavy Atom Count 18
形式电荷Formal Charge 0
复杂度Complexity 294.000
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）

象形图 GHS06,   GHS07
信号词 警告
危险声明

H413: 可能对水生生物造成长期的有害影响
预防措施声明

P273: 避免释放到环境中。

P501: 将内容物/容器处理到。。。
WGK Germany 3
RTECS NJ5903450
Merck Index 4922
个人防护装备 Eyeshields， Faceshields， Gloves， type P2 (EN 143) respirator cartridges

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批号(Lot Number) 证书类型 货号
L2312048 分析证书 I129798
E1810043 分析证书 I129798
G2525031 分析证书 I129798
E1810042 分析证书 I129798
D2521034 分析证书 I129798
B2309991 分析证书 I129798
B2309953 分析证书 I129798
B2309944 分析证书 I129798
B2309964 分析证书 I129798
B2309966 分析证书 I129798
B2309986 分析证书 I129798
J1810144 分析证书 I129798
G2410613 分析证书 I129798
G2410612 分析证书 I129798
C2429503 分析证书 I129798
C2429502 分析证书 I129798
C2429505 分析证书 I129798
C2429512 分析证书 I129798
C2223364 分析证书 I129798
G2103012 分析证书 I129798
B2309982 分析证书 I129798
J1810143 分析证书 I129798
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引用文献

1. Haifeng Ni, Sunxiang Qian, Jie Lu, Jie Feng, Xiao-zhou Mou, Jing Zhang.  (2023)  Natural Polysaccharide Delivery Platforms with Multiscale Structure Used for Cancer Chemoimmunotherapy.  MOLECULAR PHARMACEUTICS,  [PMID:37752866] [10.1021/acs.molpharmaceut.3c00633]
2. Lu Dehua, Xu Yanming, Yang Xiaodong, Li Ying, Li Mengqing, Zheng Yuanyuan, Wang Yuenan, Wang Weihu, Wang Shubin, Gao Jing, Liu Yajie.  (2023)  Neutrophil membrane-derived nanoparticle loading TLR7 agonists augments radiotherapy efficacy and boosts abscopal effect via regulating tumor microenvironment.  Cancer Nanotechnology,  14  (1): (1-18).  [10.1186/s12645-023-00193-8]
3. Hong Liu, Zhenfu Wen, Haolin Chen, Zeyu Yang, Zhicheng Le, Zhijia Liu, Yongming Chen, Lixin Liu.  (2022)  Nanoadjuvants Actively targeting lymph node conduits and blocking tumor invasion in lymphatic vessels.  JOURNAL OF CONTROLLED RELEASE,  352  (497).  [PMID:36341931] [10.1016/j.jconrel.2022.10.053]
4. Meiting Li, Yaqian Zhang, Xiaoge Zhang, Zhuoyin Liu, Junjie Tang, Miao Feng, Baizhu Chen, Dalin Wu, Jie Liu.  (2022)  Degradable Multifunctional Porphyrin-Based Porous Organic Polymer Nanosonosensitizer for Tumor-Specific Sonodynamic, Chemo- and Immunotherapy.  ACS Applied Materials & Interfaces,  14  (43): (48489–48501).  [PMID:36281484] [10.1021/acsami.2c14776]
5. Jiexin Li, He Ren, Yaping Sun, Gengqi Liu, Xingyue Yang, Qian Qiu, Yuanmeng Ding, Jonathan F. Lovell, Yumiao Zhang.  (2021)  Magnetic Metal Micelles for Enhanced Delivery of Self-Immolating CD8+ T-Cell Epitopes for Cancer Immunotherapy.  CHEMISTRY OF MATERIALS,  33  (24): (9780–9794).  [10.1021/acs.chemmater.1c03681]
6. Lili Cheng, Xiaoge Zhang, Junjie Tang, Qijun Lv, Jie Liu.  (2021)  Gene-engineered exosomes-thermosensitive liposomes hybrid nanovesicles by the blockade of CD47 signal for combined photothermal therapy and cancer immunotherapy.  BIOMATERIALS,  275  (120964).  [PMID:34147721] [10.1016/j.biomaterials.2021.120964]
7. Zhang Lirong, Zhang Jingjing, Xu Lixia, Zhuang Zijian, Liu Jingjin, Liu Suwan, Wu Yunchao, Gong Aihua, Zhang Miaomiao, Du Fengyi.  (2021)  NIR responsive tumor vaccine in situ for photothermal ablation and chemotherapy to trigger robust antitumor immune responses.  JOURNAL OF NANOBIOTECHNOLOGY,  19  (1): (1-16).  [PMID:34001148] [10.1186/s12951-021-00880-x]
8. Yuting Cao, Yan Zhou, Jinbin Pan, Xinyu Zhong, Jianmin Ding, Xiang Jing, Shao-Kai Sun.  (2021)  A general strategy towards an injectable microwave-sensitive immune hydrogel for combined percutaneous microwave ablation and immunotherapy.  CHEMICAL ENGINEERING JOURNAL,  422  (130111).  [10.1016/j.cej.2021.130111]
9. Fan Jiang, Binbin Ding, Shuang Liang, Yajie Zhao, Ziyong Cheng, Bengang Xing, Ping'an Ma, Jun Lin.  (2021)  Intelligent MoS2–CuO heterostructures with multiplexed imaging and remarkably enhanced antitumor efficacy via synergetic photothermal therapy/ chemodynamic therapy/ immunotherapy.  BIOMATERIALS,  268  (120545).  [PMID:33253965] [10.1016/j.biomaterials.2020.120545]
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