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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEML402Cat. No.: HY-104027CAS No.: 298684-44-3分式: CHClNOS分量: 295.78作靶点: Potassium Channel作通路: Membrane Transporter/Ion Channel储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 150 mg/mL (507.13
2、 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.3809 mL 16.9045 mL 33.8089 mL5 mM 0.6762 mL 3.3809 mL 6.7618 mL10 mM 0.3381 mL 1.6904 mL 3.3809 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。BIOLOGICAL ACTIVITY物活性 ML402是选择性的 TREK-1 激活剂。IC50 & Target TREK-1 1体外研究X
3、enopus oocyte two-electrode voltage-clamp measurements show that ML335 and ML402 activate K2P2.1and K2P10.1 but not K2P4.1(14.32.7 M, K2P2.1-ML335; 13.77.0 M, K2P2.1-ML402; 5.20.5 M,K2P10.1-ML335; and 5.91.6 M, K2P10.1-ML402). The K2P modulator pocket has a single difference1/2 Master of Small Molec
4、ules 您边的抑制剂师www.MedChemEamong TREK subfamily members at the cation- interaction position, K2P2.1 Lys271, which is also a lysinein K2P10.1 but a glutamine in K2P4.1.Swapping the Lys271 equivalent between K2P2.1 and K2P4.1 resultsin a clear phenotype reversal for ML335 and M402 activation. K2P2.1 (K27
5、1Q) is insensitive to ML335 andML402, whereas K2P4.1 (Q258K) responds to both with a similar EC50 to K2P2.1 (14.32.7 M, K2P2.1-ML335; 16.23.0 M, K2P4.1(Q258K)-ML335; 13.77.0 M, K2P2.1-ML402; 13.61.5 M, K2P4.1 (Q258K)-ML402) but with a lower magnitude response than K2P2.1 1.PROTOCOLKinase Assay 1 K2P
6、2.1cryst ML335 and ML402 complex crystals grow in the same conditions as K2P2.1cryst, but the proteinis incubated for at least 1 h with 2.5 mM of activator (including ML 402) before setting the crystal plates.ML335 and ML402 are insoluble in aqueous solutions, so they are dissolved in 100% DMSO at a
7、concentration of 500 mM. Then each compound is diluted 1:100 in SEC buffer to 5 mM concentration, givinga milky solution. This solution is mixed 1:1 to K2P2.1cryst previously concentrating to 12 mg/mL. TheK2P2.1cryst ML402 mixture results in a clear solution, while the mixture with ML335 is slightly
8、 milky. Thesamples are briefly centrifuged in a table-top centrifuge (10,000g) to remove any insoluble material beforesetting the crystal plates. Dose-response experiments are carried by first preparing a DMSO stock solution ofeach activator (including ML402) at a concentration of 100 mM. Owing to t
9、he low solubility of the compoundsthe highest test concentrations in recording solution are 100 M and 80 M for ML335 and ML402,respectively. Other concentrations are prepared by serial dilutions of the 100 M solution in recording buffersupplementing with 0.1% DMSO 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Lolicato M, et al. K2P2.1 (TREK-1)-activator complexes reveal a cryptic selectivity filter binding site. Nature. 2017 Jul 20;547(7663):364-368.McePdfHeightCaution: Product has not been fully validate
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