Pyr3 _TRP Channel 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPyr3Cat. No.: HY-108465CAS No.: 1160514-60-2分式: CHClFNO分量: 456.63作靶点: TRP Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling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 : 125

2、 mg/mL (273.74 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1900 mL 10.9498 mL 21.8996 mL5 mM 0.4380 mL 2.1900 mL 4.3799 mL10 mM 0.2190 mL 1.0950 mL 2.1900 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

3、剂(为保证实验结果的可靠性，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: 2.08 mg/mL (4.56 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.56 mM); Clear solution3. 请依序添加每种溶剂： 10% D

4、MSO 90% corn oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.08 mg/mL (4.56 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Pyr3是TRPC3 的选择性抑制剂，其对 TRPC3 介导的 Ca2+ 内流的 IC50 值为 700 nM。IC50 & Target IC50: 700 nM (TRPC3) 1.体外研究 Pyr3 selectively and directly inhibits TRPC3 channels among TRPC f

5、amily members. Application of Pyr3inhibits TRPC3-mediated Ca2+ influx in a dose-dependent manner with the IC50 value of 700 nM. Pyr3becomes apparent at 0.3 M, and is almost complete at 3 M. Interestingly, Ca2+ influx is inhibited by Pyr3in cells co-expressing TRPC3 plus TRPC6 but not in cells coexpr

6、essing TRPC1 plus TRPC5. The Ang II-induced NFAT translocation is suppressed by Pyr3, but weakly by Pyr2 in a concentration-dependent manner(IC50 value was 0.05 M for Pyr3 and 2 M for Pyr2) 1.PROTOCOLCell Assay 1 HEK293 cells or HEK293T cells are used throughout the study. Average time courses of Ca

7、2+ responsesinduced by 100 M UTP with Pyr3 at indicated concentrations (0.1, 1, 3, 10 M) in TRPC-transfectedHEK293 cells are tested 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Food Chem Toxicol. 2019 May 2. pii: S0278-6915(19)30260-1.S

8、ee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Kiyonaka S, et al. Selective and direct inhibition of TRPC3 channels underlies biological activities of a pyrazole compound. Proc NatlAcad Sci U S A. 2009 Mar 31;106(13):5400-5.McePdfHeightCaution: Product has not been fully validated for medical applications.Fo