CL097 是一种有效的TLR7和TLR8激动剂，可在巨噬细胞中诱导促炎细胞因子。CL097 诱导 NADPH 氧化酶启动活性，导致 fMLF 刺激的ROS产生增加。
| 生物活性 | CL097, a potentTLR7andTLR8agonist, induces pro-inflammatory cytokines in macrophages[1]. CL097 inducesNADPH oxidasepriming, resulting in an increase of the fMLF-stimulatedROSproduction[2]. |
| IC50& Target | |
体外研究
(In Vitro) | CL097 induces activation of NF-κB at 0.1 μM in TLR7 transfected HEK293 cells and at 4 μM in TLR8-transfected HEK293 cells[1].
CL097 induces hyperactivation of the NADPH oxidase by stimulating the phosphorylation of p47phox on selective sites in human neutrophils and suggest that p38 MAPK, ERK1/2, protein kinase C, and Pin1 control this process. CL097 induces the phosphorylation of p47phox on specific sites and enhances fMLF-induced p47phox phosphorylation[2].
Western Blot Analysis[2] | Cell Line: | Neutrophils | | Concentration: | 0, 0.5, 2.5, 5, and 10 μg/mL | | Incubation Time: | Pretreated for 30 minutes | | Result: | Induced phosphorylation of p47phox on specific sites in a concentration-dependent manner. |
|
体内研究
(In Vivo) | CL097 and CD40 agonist stimulation induces efficient diabetogenic Cytotoxic T lymphocyte (CTL) function in NOD mice. CL097 (5 mg/kg, s.c.) alone causes a modest specific lysis of the target peptide (~25%). However, treatment with a combination of CL097 and CD40 agonist (10 mg/kg, i.p.) results in an increase of approximately twofold in the specific lysis of the IGRP-peptide-coated targets compared with CL097 treatment alone[3].
| Animal Model: | Female 8.3 NOD mice (5-6 weeks old)[3] | | Dosage: | 5 mg/kg | | Administration: | Injected s.c. | | Result: | Caused a modest specific lysis of the target peptide (~25%). |
|
| 分子量 | |
| 性状 | |
| Formula | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(358.76 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.5876 mL | 17.9379 mL | 35.8757 mL | | 5 mM | 0.7175 mL | 3.5876 mL | 7.1751 mL | | 10 mM | 0.3588 mL | 1.7938 mL | 3.5876 mL |
*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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (8.97 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.97 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (8.97 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.97 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (8.97 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.97 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
|
