1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECa2+ channel agonist 1Cat. No.: HY-41076CAS No.: 1402821-24-2分式: CHNO分量: 354.45作靶點(diǎn): Calcium Channel; CDK作通路: Membrane Transporter/Ion Channel; Neuronal Signaling; CellCycle/DNA Damage儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent

2、-80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (141.06 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.05 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.05 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOL

3、OGICAL ACTIVITY物活性 Ca2+ channel agonist 1種 N-型鈣離通道 (N-type Ca2+ channel) 激動(dòng)劑和 Cdk2 的抑制劑，EC50 分別為 14.23 M 和 3.34 M，對(duì)運(yùn)動(dòng)神經(jīng)終端功能障礙有潛在療效。IC50 & Target CDK2 N-Type Ca2+ Channel3.34 M (EC50) 14.23 M (EC50)體外研究 Ca2+ channel agonist 1 (Compound 13d) is an agonist of N-type Ca2+ channel and an inhibitor of Cdk

4、2, withEC50s of 14.23 M and 3.34 M, respectively. Ca2+ channel agonist 1 exhibits a ca. 2-fold increasedagonism and a 22-fold decreased cdk2 kinase activity versus the standard, (R)-roscovitine 1.PROTOCOLCell Assay 1 Briefly, the pipet solution consists of 70 nM Cs2SO4, 60 mM CsCl, 1 mM MgCl2, and 1

5、0 mM HEPES at pH7.4. Cultured cells are bathed in a saline composed of 130 mM choline chloride (ChCl), 10 mMtetraethylammonium chloride (TEA-Cl), 2 mM CaCl2, 1 mM MgCl2, and 10 mM HEPES at pH 7.4. Patchpipettes are fabricated from borosilicate glass, and capacitive currents and passive membrane resp

6、onses tovoltage commands are subtracted. Currents are amplified by an amplifier, filtered at 5 kHz, and digitized at10 kHz for subsequent analysis. A liquid junction potential of 11.3 mV is subtracted during recordings. Tomeasure effects on calcium channel tail currents, the tail current integral is

7、 measured before and afterapplication of a derivative (including Ca2+ channel agonist 1), with the integral of each trace beingnormalized to its peak.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Liang M, et al. Synthesis and biological evaluation of a selective N- and p/q-type calcium channel agonist. ACS Med Chem Lett. 2012Oct 1;3(12):985-990.McePdfHeightCaution: Product has not been fully validated for medical applications.For rese