CU-CPD107
目录号 : GC25314CU-CPD107 is a selective, dual-activity small-molecule which demonstrated differential activity against the TLR8 agonists and ssRNA ligands.
Cas No.:2573912-32-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.50%
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- SDS (Safety Data Sheet)
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CU-CPD107 is a selective, dual-activity small-molecule which demonstrated differential activity against the TLR8 agonists and ssRNA ligands. In the presence of R848, CU-CPD107 acts as a TLR8 signaling inhibitor (IC50=13.7 μM). In the presence of ssRNA, CU-CPD107 shows synergistic agonist activities, while CU-CPD107 alone is unable to influence TLR8 signaling.
CU-CPD107, a tetrasubstituted imidazole, inhibits R848-induced TLR8 signaling and shows unexpected synergistic agonist activities in the presence of ssRNA, while CU-CPD107 alone is unable to influence TLR8 signaling.[1]
[1] Yang Y, et al. Nat Commun. 2021 Jul 16;12(1):4351.
Cas No. | 2573912-32-8 | SDF | Download SDF |
分子式 | C16H21IN2O2 | 分子量 | 400.26 |
溶解度 | DMSO: 80 mg/mL (199.87 mM);Water: Insoluble;Ethanol: 80 mg/mL (199.87 mM) | 储存条件 | Store at -20°C |
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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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.4984 mL | 12.4919 mL | 24.9838 mL |
5 mM | 0.4997 mL | 2.4984 mL | 4.9968 mL |
10 mM | 0.2498 mL | 1.2492 mL | 2.4984 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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。
Tetrasubstituted imidazoles as incognito Toll-like receptor 8 a(nta)gonists
Nat Commun 2021 Jul 16;12(1):4351.PMID:34272380DOI:PMC8285539
Small-molecule modulators of TLR8 have drawn much interests as it plays pivotal roles in the innate immune response to single-stranded RNAs (ssRNAs) derived from viruses. However, their clinical uses are limited because they can invoke an uncontrolled, global inflammatory response. The efforts described herein culminate in the fortuitous discovery of a tetrasubstituted imidazole CU-CPD107 which inhibits R848-induced TLR8 signaling. In stark contrast, CU-CPD107 shows unexpected synergistic agonist activities in the presence of ssRNA, while CU-CPD107 alone is unable to influence TLR8 signaling. CU-CPD107's unique, dichotomous behavior sheds light on a way to approach TLR agonists. CU-CPD107 offers the opportunity to avoid the undesired, global inflammation side effects that have rendered imidazoquinolines clinically irrelevant, providing an insight for the development of antiviral drugs.