Pyr3 _TRP Channel 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPyr3Cat. No.: HY-108465CAS No.: 1160514-60-2分式: CHClFNO分量: 456.63作靶點(diǎn): TRP Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 125

2、 mg/mL (273.74 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助?/p>

3、劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)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: 2.08 mg/mL (4.56 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.56 mM); Clear solution3. 請依序添加每種溶劑： 10% D

4、MSO 90% corn oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL (4.56 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Pyr3是TRPC3 的選擇性抑制劑，其對 TRPC3 介導(dǎo)的 Ca2+ 內(nèi)流的 IC50 值為 700 nM。IC50 & Target IC50: 700 nM (TRPC3) 1.體外研究 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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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