CaCCinh-A01 - Chloride Channel 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECaCCinh-A01Cat. No.: HY-100611CAS No.: 407587-33-1分式: CHNOS分量: 347.43作靶点: Chloride 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 : 50 mg/mL (143.

2、91 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.8783 mL 14.3914 mL 28.7828 mL5 mM 0.5757 mL 2.8783 mL 5.7566 mL10 mM 0.2878 mL 1.4391 mL 2.8783 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，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠

3、性，体内实验的作液，建议您现现配，当天使；澄清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 (7.20 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.20 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn o

4、il1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (7.20 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 CaCCinh-A01是TMEM16A 和钙激活氯化物通道 (CaCC) 的抑制剂，IC50 值分别为 2.1 和 10 M。IC50 & Target IC50: 2.1 M (TMEM16A) 1, 10 M (CaCC) 2体外研究 30 M CaCCinh-A01 and 100 M tannic acid strongly inhibit CaC

5、C current following ATP stimulation 1.Calcium-dependent chloride current is reduced by 3814, 6610, and 911% by 0.1, 1, and 10 M CaCCinh-A01, respectively. ATP-induced short-circuit currents are reduced by 387 and 783% at 10 and 30 MCaCCinh-A01, respectively 2.PROTOCOLCell Assay 1 Each well of a 96-w

6、ell plate is washed three times with PBS (200 L/wash), leaving 50 L of PBS. Testcompounds (including CaCCinh-A01) (0.5 L) are added to each well at 25 M final concentration. After 10min, 96-well plates are transferred to a plate reader for fluorescence assay. Each well is assayed individuallyfor TME

7、M16A-mediated I- influx by recording fluorescence continuously (400 ms/point) for 2 s (base line),then 50 L of a 140 mM I- solution containing 200 M ATP is added. The initial rate of I- influx is computedfrom fluorescence data by nonlinear regression 1.MCE has not independently confirmed the accurac

8、y of these methods. They are for reference only.REFERENCES1. TMEM16A inhibitors reveal TMEM16A as a minor component of calcium-activated chloridechannel conductance in airway and intestinalepithelial cells. J Biol Chem. 2011 Jan 21;286(3):2365-74.2. De La Fuente R, et al. Small-molecule screen identifies inhibitors of a human intestinal calcium-activated chloridechannel. MolPharmacol. 2008 Mar;73(3):758-68.McePdfHeightCaution: Product has not been fully validated for medical applic