Gardiquimod
(Synonyms: 4-氨基-2-[(乙基氨基)甲基]-ALPHA,ALPHA-二甲基-1H-咪唑并[4,5-C]喹啉-1-乙醇) 目录号 : GC14864A selective agonist of human TLR7
Cas No.:1020412-43-4
Sample solution is provided at 25 µL, 10mM.
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Gardiquimod is an agonist of human toll-like receptor 7 (TLR7) [1][2].
Toll-like receptors (TLRs) are a family of highly conserved pattern recognition receptors involved in innate immune responses to pathogen infection. TLR7 is highly expressed by plasmacytoid dendritic cells, and is also found on other leukocyte subpopulations. TLR7 and TLR8 recognize single-stranded RNA from viruses [4].
Gardiquimod is an agonist of human toll-like receptor 7 (TLR7), but not human TLR8, although it activates both porcine TLR7 and TLR8. In transfected 293T cells, Gardiquimod preferentially activated porcine TLR8 (pTLR8) [1]. Gardiquimod is a member of imidazoquinoline family. When codelivered intranasally with plant-derived Norwalk virus virus-like particles (NV VLPs), gardiquimod (GARD) induced NV VLP-specific serum IgG and IgG isotype responses and mucosal IgA responses in the gastrointestinal, respiratory, and reproductive tracts [3]. In macrophages and activated peripheral blood mononuclear cells (PBMCs) infected with X4, R5 or dual-tropic (R5/X4) strains of HIV-1, Gardiquimod inhibited HIV-1 reverse transcriptase and significantly reduced infection. Gardiquimod also induced interferon-alpha (IFN-a) transcription and sustained IFN-a protein secretion [4]. In BxPC-3 cells, Gardiquimod inhibited cell proliferation and migration, and induced apoptosis [5].
In C57BL/6 mice, Gardiquimod enhanced the ability of Treg cell to suppress the proliferation of Tresp cells. The CD4+CD25+Treg cells from mice that had received gardiquimod exhibited an increased inhibitory effect on anti-CD3/anti-CD28 mAb-coated bead-stimulated Tresp cells [2].
References:
[1]. Zhu J, Lai K, Brownile R, et al. Porcine TLR8 and TLR7 are both activated by a selective TLR7 ligand, imiquimod. Mol Immunol. 2008 Jun;45(11):3238-43.
[2]. Forward NA1, Furlong SJ, Yang Y, et al. Signaling through TLR7 enhances the immunosuppressive activity of murine CD4+CD25+ T regulatory cells. J Leukoc Biol. 2010 Jan;87(1):117-25.
[3]. Velasquez LS, Hjelm BE, Arntzen CJ, et al. An intranasally delivered Toll-like receptor 7 agonist elicits robust systemic and mucosal responses to Norwalk virus-like particles. Clin Vaccine Immunol. 2010 Dec;17(12):1850-8.
[4]. Buitendijk M, Eszterhas SK, Howell AL. Gardiquimod: a Toll-like receptor-7 agonist that inhibits HIV type 1 infection of human macrophages and activated T cells. AIDS Res Hum Retroviruses. 2013 Jun;29(6):907-18.
[5]. Zou BB, Wang F, Li L, et al. Activation of Toll-like receptor 7 inhibits the proliferation and migration, and induces the apoptosis of pancreatic cancer cells. Mol Med Rep. 2015 Oct;12(4):6079-85.
| Cas No. | 1020412-43-4 | SDF | |
| 别名 | 4-氨基-2-[(乙基氨基)甲基]-ALPHA,ALPHA-二甲基-1H-咪唑并[4,5-C]喹啉-1-乙醇 | ||
| 化学名 | 4-amino-2-[(ethylamino)methyl]-α,α-dimethyl-1H-imidazo[4,5-c]quinoline-1-ethanol | ||
| Canonical SMILES | NC1=NC2=C(C3=C1N=C(CNCC)N3CC(C)(O)C)C=CC=C2 | ||
| 分子式 | C17H23N5O | 分子量 | 313.4 |
| 溶解度 | ≤12mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1908 mL | 15.9541 mL | 31.9081 mL |
| 5 mM | 0.6382 mL | 3.1908 mL | 6.3816 mL |
| 10 mM | 0.3191 mL | 1.5954 mL | 3.1908 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet