Gardiquimod trifluoroacetate
目录号 : GC33910
A selective agonist of human TLR7
Cas No.:1159840-61-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | Peripheral blood cells (PBMCs) are resuspended at a concentration of 5×106 cells/mL in serum-free RPMI and added to large (150-cm2) tissue culture flasks to permit monocyte attachment. The cells are maintained in a humidified incubator at 37°C with 5% CO2 for a total of 8 days. On the fifth day of culture, the medium is refreshed and one-half of the cells are treated with 0.6 to 3.0 μM Gardiquimod trifluoroacetate for 3 days prior to infection with HIV-1 on day 8 of culture. Control macrophages are left untreated[1]. |
Animal experiment: | Six- to eight-week-old C57BL/6 mice weighing 20 to 24 g are used in this study. For subcutaneous (s.c.) tumors, 5×104 B16 cells in 100 µL of PBS are injected s.c. into the right flank of C57BL/6 mice on day 0. Mice are vaccinated intravenously with 4×104 DCs on day 7 and peritumorally injected with 1 mg/kg Gardiquimod trifluoroacetate on days 8 and 10. Control mice are injected with an equivalent volume of PBS. Beginning on day 8, the tumor length and width are measured with a vernier caliper, and tumor volume is calculated as length×width2/2. The mice are killed on day 13, and tumors are excised and weighed[2]. |
References: [1]. Buitendijk M, et 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. | |
Gardiquimod is an agonist of human toll-like receptor 7 (TLR7), but not human TLR8, although it activates both porcine TLR7 and TLR8.1 At 0.5 to 2 ?g/ml, it enhances the immunosuppressive activity of T regulatory cells.2 Gardiquimod is effective as a mucosal adjuvant for Norwalk virus-like particles and inhibits infection of macrophages and T cells by HIV-1.3,4 It inhibits proliferation and migration while inducing apoptosis in pancreatic cancer cells in vitro.5
1.Zhu, J., Lai, K., Bronile, R., et al.Porcine TLR8 and TLR7 are both activated by a selective TLR7 ligand, imiquimodMol. Immunol.45(11)3238-3243(2008) 2.Forward, N.A., Furlong, S.J., Yang, Y., et al.Signaling through TLR7 enhances the immunosuppressive activity of murine CD4+CD25+ T regulatory cellsJ. Leukoc. Biol.87(1)117-125(2010) 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 particlesClin. Vaccine Immunol.17(12)1850-1858(2010) 4.Buitendijk, M., Eszterhas, S.K., and Howell, A.L.Gardiquimod: A toll-like receptor-7 agonist that inhibits HIV type 1 infection of human macrophages and activated T cellsAIDS Res. Hum. Restroviruses29(6)907-918(2013) 5.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 cellsMol. Med. Rep.12(4)6079-6085(2015)
| Cas No. | 1159840-61-5 | SDF | |
| Canonical SMILES | OC(C)(C)CN1C(CNCC)=NC2=C1C3=CC=CC=C3N=C2N.FC(C(O)=O)(F)F.FC(C(O)=O)(F)F | ||
| 分子式 | C21H25F6N5O5 | 分子量 | 541.44 |
| 溶解度 | DMSO : 100 mg/mL (184.69 mM) | 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 | 1.8469 mL | 9.2346 mL | 18.4693 mL |
| 5 mM | 0.3694 mL | 1.8469 mL | 3.6939 mL |
| 10 mM | 0.1847 mL | 0.9235 mL | 1.8469 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。