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 : GC14864
一键复制产品信息
Gardiquimod是一种Toll样受体7（TLR7）激动剂，能够抑制HIV1型感染人类巨噬细胞和活化T细胞。
Cas No.:1020412-43-4
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Gardiquimod is a Toll-like receptor 7 (TLR7) agonist that inhibits HIV-1 infection of human macrophages and activation of T cells[1, 2]. When combined with plant-derived norovirus virus-like particles (NVVLPs) and administered intranasally, Gardiquimod induces NVVLP-specific serum IgG and its subtype responses and mucosal IgA responses in the gastrointestinal, respiratory, and reproductive tracts[3].
In vitro, treatment of mouse spleen cells with Gardiquimod (0-2.5µg/mL) for 48h significantly induced cell proliferation[4]. Treatment of RAW264.7 mouse macrophages with Gardiquimod (1µg/mL) for 24h significantly induced the expression of CD40, CD80, and CD86[4]. Pretreatment of HaCaT cells with Gardiquimod (2µg/mL) for 2h downregulated the expression of Ca2+-induced differentiation markers and activated the Raf-MEK-ERK and PI3K-AKT signaling pathways in HaCaT cells[5]. Gardiquimod (3µg/mL) treatment of the human pancreatic adenocarcinoma cell line BxPC-3 inhibited cell proliferation and migration, induced apoptosis, downregulated the expression levels of cyclin B1, cyclin E, and B-cell lymphoma 2, and upregulated the expression of B-cell-associated X protein[6].
In vivo, subcutaneous B16 melanoma model mice treated with Gardiquimod (1mg/kg) via peritumoral injection twice, combined with a dendritic cell (DC) vaccine, significantly inhibited tumor growth[4].
References:
[1] Buitendijk M, Eszterhas S K, Howell A L. Gardiquimod: a Toll-like receptor-7 agonist that inhibits HIV type 1 infection of human macrophages and activated T cells[J]. AIDS research and human retroviruses, 2013, 29(6): 907-918.
[2] Goyal D K, Keshav P, Kaur S. Adjuvant effects of TLR agonist gardiquimod admixed with Leishmania vaccine in mice model of visceral leishmaniasis[J]. Infection, Genetics and Evolution, 2021, 93: 104947.
[3] Velasquez L S, Hjelm B E, Arntzen C J, et al. An intranasally delivered Toll-like receptor 7 agonist elicits robust systemic and mucosal responses to Norwalk virus-like particles[J]. Clinical and Vaccine Immunology, 2010, 17(12): 1850-1858.
[4] Ma F, Zhang J, Zhang J, et al. The TLR7 agonists imiquimod and gardiquimod improve DC-based immunotherapy for melanoma in mice[J]. Cellular & molecular immunology, 2010, 7(5): 381-388.
[5] Jia B, Luo X, Cheng F W, et al. Gardiquimod inhibits the expression of calcium-induced differentiation markers in HaCaT cells[J]. Molecular biology reports, 2013, 40(11): 6363-6369.
[6] Zou B B, 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[J]. Molecular medicine reports, 2015, 12(4): 6079-6085.
Gardiquimod是一种Toll样受体7（TLR7）激动剂，能够抑制HIV1型感染人类巨噬细胞和活化T细胞[1, 2]。Gardiquimod与植物源诺如病毒病毒样颗粒（NV VLPs）联合鼻内给药时，能够诱导胃肠道、呼吸道和生殖道产生NV VLP特异性血清IgG及其亚型应答和黏膜IgA应答[3]。
在体外，Gardiquimod（0-2.5µg/mL）处理小鼠脾细胞48h，显著诱导了细胞增殖[4]。Gardiquimod（1µg/mL）处理RAW264.7小鼠巨噬细胞24h，显著诱导了CD40、CD80和CD86的表达[4]。Gardiquimod（2µg/mL）预处理HaCaT细胞2h，下调了Ca2+诱导的分化标志物表达，激活了HaCaT细胞中的 Raf-MEK-ERK和PI3K-AKT信号通路[5]。Gardiquimod（3µg/mL）处理人胰腺腺癌细胞系BxPC-3细胞，抑制了细胞增殖和迁移，诱导了细胞凋亡，下调了细胞周期蛋白B1、细胞周期蛋白E和B细胞淋巴瘤2的表达水平，上调了B细胞相关X蛋白的表达[6]。
在体内，Gardiquimod（1mg/kg）通过肿瘤周围注射给药治疗皮下B16黑色素瘤模型小鼠2次，联合树突状细胞（DC）疫苗可显著抑制肿瘤的生长[4]。
| Cell experiment [1]: | |
Cell lines | Splenocytes from C57BL/6 mice |
Preparation Method | Proliferation was determined by culturing 5×104 freshly isolated splenocytes from C57BL/6 mice with 0-2.5µg/mL imiquimod or Gardiquimod in 96-well plates for 48h. MTT (20mL, 5mg/mL) was added 4h before the end of the incubation period. DMSO was used to dissolve granules, and the absorbance at 570nm of each sample was determined with a microplate autoreader. |
Reaction Conditions | 0-2.5µg/mL; 48h |
Applications | Both agonists promoted the proliferation of lymphocytes with a greater effect at the dosage of 1.25mg/ml, and Gardiquimod seemed to be more efficient than imiquimod. |
| Animal experiment [1]: | |
Animal models | C57BL/6 mice |
Preparation Method | C57BL/6 mice were inoculated with 53104 B16 cells. On day 7, mice received an intravenous infusion of 4×104 dendritic cells (DCs), and on days 8 and 10, mice received 1mg/kg of either Gardiquimod or imiquimod by peritumoral injection. Control mice were injected with an equivalent volume of PBS. The tumor volumes were calculated and the growth curves of melanomas in treated mice were determined. The treated mice were killed on day 13, and tumors were weighed. The tumor tissues were analyzed by hematoxylin and eosin staining. |
Dosage form | 1mg/kg; peritumoral injection |
Applications | Combination therapy with Gardiquimod or imiquimod and DC vaccine inhibits the growth of subcutaneous B16 melanomas. |
References: | |
| 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1908 mL | 15.9541 mL | 31.9081 mL |
| 5 mM | 638.2 μL | 3.1908 mL | 6.3816 mL |
| 10 mM | 319.1 μL | 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet