TLR7/8 agonist 1 dihydrochloride
目录号 : GC30516
A dual agonist of TLR7 and TLR8
Cas No.:1620278-72-9
Sample solution is provided at 25 µL, 10mM.
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TLR7/8 agonist 1 is a dual agonist of toll-like receptor 7 (TLR7) and TLR8 (EC50s = 50 and 55 nM, respectively, in cell-based assays).1 It increases the levels of TNF-α, IFN-γ, IL-12p40, and chemokine (C-C motif) ligand 4 (CCL4) in human peripheral blood mononuclear cells (PBMCs) in a biphasic manner. TLR7/8 agonist 1 (25 nmol, s.c.) increases serum levels of IL-12p40 and chemokine (C-X-C motif) ligand 10 (CXCL10), as well as the number of dendritic cells per injection-site proximal lymph node, in mice.2 It has been conjugated to various fluorophores as TLR7 probes and to polymer particles for the modulation of TLR7/8 agonist 1 adjuvant activity.3,2
1.Beesu, M., Caruso, G., Salyer, A.C., et al.Structure-based design of human TLR8-specific agonists with augmented potency and adjuvanticityJ. Med. Chem.58(19)7833-7849(2015) 2.Lynn, G.M., Chytil, P., Francica, J.R., et al.Impact of polymer-TLR-7/8 agonist (adjuvant) morphology on the potency and mechanism of CD8 T cell inductionBiomacromolecules20(2)854-870(2019) 3.Shukla, N.M., Mutz, C.A., Ukani, R., et al.Syntheses of fluorescent imidazoquinoline conjugates as probes of Toll-like receptor 7Bioorg. Med. Chem. Lett.20(22)6384-6386(2010)
Cell experiment: | Fresh human peripheral blood mononuclear cells (hPBMC) are used. Aliquots of PBMCs (105 cells in 100 μL/well) are stimulated for 12 h with graded concentrations of test compounds (e.g., TLR7/8 agonist 1; 0.1, 1, 10, and 100 μg/mL). Supernatants are isolated by centrifugation and are assayed in duplicates using analyte-specific multiplexed cytokine/chemokine bead array assays[2]. |
References: [1]. Shukla NM, et al. Syntheses of fluorescent imidazoquinoline conjugates as probes of Toll-like receptor 7. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6384-6. | |
| Cas No. | 1620278-72-9 | SDF | |
| Canonical SMILES | NC1=NC2=CC=CC=C2C3=C1N=C(CCCC)N3CC4=CC=C(CN)C=C4.[H]Cl.[H]Cl | ||
| 分子式 | C22H27Cl2N5 | 分子量 | 432.39 |
| 溶解度 | DMSO : 83.33 mg/mL (192.72 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 | 2.3127 mL | 11.5636 mL | 23.1273 mL |
| 5 mM | 0.4625 mL | 2.3127 mL | 4.6255 mL |
| 10 mM | 0.2313 mL | 1.1564 mL | 2.3127 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet