C-170
目录号 : GC46983
A STING inhibitor
Cas No.:346691-38-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
C-170 is an inhibitor of stimulator of interferon genes (STING).1,2 It binds to STING, inhibits its palmitoylation, and prevents the recruitment and phosphorylation of TBK1.1 It selectively reduces human and mouse STING-, but not RIG-I- or TBK1-, mediated IFN-β reporter activity in HEK293 cells when used at concentrations ranging from 0.02 to 2 µM.
1.Haag, S.M., Gulen, M.F., Reymond, L., et al.Targeting STING with covalent small-molecule inhibitorsNature559(7713)269-273(2018) 2.Zhang, H., You, Q.-D., and Xu, X.-L.Targeting stimulator of interferon genes (STING): A medicinal chemistry perspectiveJ. Med. Chem.63(8)3785-3816(2019)
| Cas No. | 346691-38-1 | SDF | |
| Canonical SMILES | CCCCC1=CC=C(NC(C2=CC=C([N+]([O-])=O)O2)=O)C=C1 | ||
| 分子式 | C15H16N2O4 | 分子量 | 288.3 |
| 溶解度 | DMSO : 125 mg/mL (433.58 mM; Need ultrasonic) | 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 | 3.4686 mL | 17.343 mL | 34.6861 mL |
| 5 mM | 0.6937 mL | 3.4686 mL | 6.9372 mL |
| 10 mM | 0.3469 mL | 1.7343 mL | 3.4686 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。
Novel CRBN-Recruiting Proteolysis-Targeting Chimeras as Degraders of Stimulator of Interferon Genes with In Vivo Anti-Inflammatory Efficacy
J Med Chem 2022 May 12;65(9):6593-6611.PMID:35452223DOI:10.1021/acs.jmedchem.1c01948.
The activation of the cyclic GMP-AMP synthase-stimulator of interferon gene (STING) pathway has been associated with the pathogenesis of many autoimmune and inflammatory disorders, and small molecules targeting STING have emerged as a new therapeutic strategy for the treatment of these diseases. While several STING inhibitors have been identified with potent anti-inflammatory effects, we would like to explore STING degraders based on the proteolysis-targeting chimera (PROTAC) technology as an alternative strategy to target the STING pathway. Thus, we designed and synthesized a series of STING protein degraders based on a small-molecule STING inhibitor (C-170) and pomalidomide (a CRBN ligand). These compounds demonstrated moderate STING-degrading activities. Among them, SP23 achieved the highest degradation potency with a DC50 of 3.2 μM. Importantly, SP23 exerted high anti-inflammatory efficacy in a cisplatin-induced acute kidney injury mouse model by modulating the STING signaling pathway. Taken together, SP23 represents the first PROTAC degrader of STING deserving further investigation as a new anti-inflammatory agent.
Polybenzimidazole/Mxene composite membranes for intermediate temperature polymer electrolyte membrane fuel cells
Nanotechnology 2018 Jan 19;29(3):035403.PMID:29135464DOI:10.1088/1361-6528/aa9ab0.
This report demonstrated the first study on the use of a new 2D nanomaterial (Mxene) for enhancing membrane performance of intermediate temperature (>100 °C) polymer electrolyte membrane fuel cells (ITPEMFCs). In this study, a typical Ti3C2T x -MXene was synthesized and incorporated into polybenzimidazole (PBI)-based membranes by using a solution blending method. The composite membrane with 3 wt% Ti3C2T x -MXene showed the proton conductivity more than 2 times higher than that of pristine PBI membrane at the temperature range of 100 °C-170 °C, and led to substantial increase in maximum power density of fuel cells by ∼30% tested at 150 °C. The addition of Ti3C2T x -MXene also improved the mechanical properties and thermal stability of PBI membranes. At 3 wt% Ti3C2T x -MXene, the elongation at break of phosphoric acid doped PBI remained unaffected at 150 °C, and the tensile strength and Young's modulus was increased by ∼150% and ∼160%, respectively. This study pointed out promising application of MXene in ITPEMFCs.
Thermal stability and gas absorption characteristics of ionic liquid-based solid polymer electrolytes
J Chem Phys 2021 Feb 7;154(5):054902.PMID:33557536DOI:10.1063/5.0037978.
Ionic liquid (IL)-based solid polymer electrolytes (SPE) with stable thermal properties and low electrical resistivity have been evaluated. Two candidates for the polymer component of the SPE, poly(ethylene glycol) diacrylate (PEGDA) and Nafion, were considered. Differential scanning calorimetry analysis and electrical resistivity tests revealed that PEGDA, in comparison to Nafion, enables the formation of uniform SPEs with lower electrical resistivity and better thermal stability within a range of 25 °C-170 °C. Therefore, PEDGA was selected for further evaluation of the IL component effect on the resulting SPE. Six IL candidates, including 1-butyl-3-methylimidazolium methanesulfonate ± methanesulfonic acid (BMIM.MS ± MSA), diethylmethylammonium triflate ±bis(trifluoromethanesulfonyl)imine (Dema.OTF±HTFSI), and 1-butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide ± bis(trifluoromethanesulfonyl)imine (BMIM.TFSI ± HTFSI), were selected to test the effect of hydrophobicity/hydrophilicity of the IL on the resulting SPE. Fourier transformation infrared spectrometer analysis revealed that the BMIM.MSA-based electrolytes have the highest tendency to absorb from the environment and keep the moisture, while Dema.OTF has the fastest curing time. The SPE candidates were further evaluated for absorption characteristics of different gasses and vapors, such as N2, O2, ethanol vapor, and diluted CO/N2, that were tested with the in situ quartz crystal microbalance (QCM) technique. Among all six candidates, BMIM.MS showed the largest N2 and O2 absorption capacity from the environment. Dema.OTF + HTFSI, meanwhile, demonstrated a higher level of interactions with the ethanol vapor. In the case of CO/N2, QCM analysis revealed that BMIM.MS+MSA has the largest, ∼13 µg/cm2, absorption capacity that is reached within 400 s of being exposed to the gas mixture.