CU-CPT-8m-TLR8-specific-antagonist-DataSheet-生命科學試劑-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作靶點: Toll-like Receptor (TLR)作通路: Immunology/Inflammation儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶

2、解性數(shù)據(jù)體外實驗 DMSO : 30 mg/mL (118.92 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄的儲備液，再依次添加助溶?為保證實

3、驗結果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (9.91 mM); Suspended solution; Need ultrasonic and warming2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 1.25 mg/mL (4.96 mM); Clear so

4、lution; Need ultrasonic and warming3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (9.91 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 CU-CPT-8mTLR8 的特異性拮抗劑，其 IC50 值為 67 nM。IC50 & Target TLR867 nM (IC50)體外研究 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