ST034307 _Adenylate Cyclase 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEST034307Cat. No.: HY-101279CAS No.: 133406-29-8分式: CHClO分量: 297.95作靶点: Adenylate Cyclase作通路: GPCR/G Protein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 (167.81 mM; Need ultrason

2、ic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.3563 mL 16.7813 mL 33.5627 mL5 mM 0.6713 mL 3.3563 mL 6.7125 mL10 mM 0.3356 mL 1.6781 mL 3.3563 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 ST034307种有效的，选择性的 adenylyl cyclase 1 抑制剂，IC50 值为 2.3 M。IC50 & Targe

3、t IC50: 2.3 M (AC1) 1体外研究ST034307 reveals selective inhibition of AC1 and potentiates AC8 activity to a nonsignificant small extent.ST034307 potentiates phorbol 12-myristate 13-acetate (PMA)-stimulated cAMP production by AC2.ST034307 significantly inhibits the forskolin- or isoproterenol-stimulated

4、AC1 activity in HEK cells stably1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEexpressing AC1. In contrast, ST034307 has no significant effects in the wild-type HEK cells. ST034307significantly inhibits the Ca2+/calmodulin-stimulated cAMP accumulation in the hippocampal homogenates.ST034307 dose-d

5、ependently inhibits both the development and the maintenance of MOR-mediatedsensitization of AC1 1.体内研究 ST034307 (0.25 g) causes a significant relief of CFA-induced inflammatory pain in mice. ST034307 exhibitsan estimated median effective dose (E50) value for analgesia of 0.28 g in the mouse pain mo

6、del 1.PROTOCOLCell Assay 1 Cell viability assays are conducted with HEK-AC1 cells following plating and compound incubation protocolsidentical to the procedures described in “cAMP accumulation in cells.” Cell viability is measured as apercentage of vehicle using 2% Triton X-100 as a control. The Cel

7、lTiter-Glo Luminescent Cell Viability Assaykit from Promega is used to assess cell viability according to the manufacturers instructions. Luminescencecounts are measured using Synergy 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Brust TF, et al. Identification of a selective small-molecule inhibitor of type 1 adenylyl cyclase activity with analgesic properties. SciSignal. 2017 Feb 21;10(467).McePdfHeightCaution: Product has not been fully validated for medical applications.For re