CU-CPT-8m-TLR8-specific-antagonist-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECU-CPT-8mCat. No.: HY-112050CAS No.: 125079-83-6Synonyms: TLR8-specific antagonist分式: CHNO分量: 252.27作靶点: Toll-like Receptor (TLR)作通路: Immunology/Inflammation储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶

2、解性数据体外实验 DMSO : 30 mg/mL (118.92 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.9640 mL 19.8200 mL 39.6401 mL5 mM 0.7928 mL 3.9640 mL 7.9280 mL10 mM 0.3964 mL 1.9820 mL 3.9640 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，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实

3、验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (9.91 mM); Suspended solution; Need ultrasonic and warming2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 1.25 mg/mL (4.96 mM); Clear so

4、lution; Need ultrasonic and warming3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (9.91 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 CU-CPT-8mTLR8 的特异性拮抗剂，其 IC50 值为 67 nM。IC50 & Target TLR867 nM (IC50)体外研究 CU-CPT-8m is a specific TLR8 antagonis

5、t, with an IC50 of 6710 nM and negligible cytotoxicity. The Kdvalue of CU-CPT-8m is determined to be 220 nM. CU-CPT-8m only reduces the proinflammatory response inthe TLR8-overexpressing cells strongly supports that CU-CPT-8m directly recognizes TLR8 in cells. It isparticularly notable that TLR7 sig

6、naling is not affected at concentrations up to 75 M. TLR7 and TLR8 areclosely related and share many common ligands. Treatment of 1 M CU-CPT-8m completely abolishes theelevation of TNF- and IL-8 mRNA levels induced by R848. CU-CPT-8m inhibits R848-induced TNF-production in the differentiated THP-1 m

7、onocytes cells in a dose-dependent manner with an IC50 of 9010nM, which is in good agreement with its IC50 value determined in HEK-Blue TLR8 cells 1.REFERENCES1. Zhang S, et al. Small-molecule inhibition of TLR8 through stabilization of its resting state. Nat Chem Biol. 2018 Jan;14(1):58-64.McePdfHeightCaution: Product has not been fully validated for medical applications.For research u