PSI-697-P-Selectin-Inhibitor-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPSI-697Cat. No.: HY-15526CAS No.: 851546-61-7Synonyms: P-Selectin Inhibitor分式: CHClNO分量: 367.83作靶点: Others作通路: Others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 : 45.8 mg/mL (124.51 mM)*

2、means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.7186 mL 13.5932 mL 27.1865 mL5 mM 0.5437 mL 2.7186 mL 5.4373 mL10 mM 0.2719 mL 1.3593 mL 2.7186 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 PSI-697种服的 P-selectin 抑制剂，IC50 值为 125 M 1。IC

3、50 & Target IC50: 125 M (P-selectin) 1体外研究PSI-697 inhibits the binding of a soluble human P-selectin to PSGL-1, in a reproducible concentration-1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEdependent manner inhibiting 50% of binding at a concentration of 125 M in vitro 1.体内研究 PSI-697 (0-50 mg/kg;

4、 p.o.) significantly reduces the number of rolling leukocytes by 39% versus vehiclecontrol 1.PSI-697 (100 mg/kg; p.o.) reduces thrombus weight by 18% relative to vehicle, without prolonging bleedingtime in a rat venous thrombosis model 1.PSI-697 (30 mg/kg; p.o.; daily; 6 days) promotes thrombus reso

5、lution and decreases inflammation in ababoon model of venous thrombosis 2.PSI-697 (30 mg/kg; i.g.; daily) decreases vein wall injury in a rat stenosis model of venous thrombosis 2.Animal Model: 4-5 weeks male Sprague-Dawley rat (50-100 g) 1Dosage: 0 mg/kg, 30 mg/kg, 50 mg/kgAdministration: Oral admi

6、nistrationResult: At an oral dose of 50 mg/kg reduced the number of rolling leukocytes by 39% versusvehicle control.户使本产品发表的科研献 Oncogene. 2019 Mar;38(12):2005-2019.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. 1. Bedard PW et al. Characterization of the novel P-selectin inhib

7、itor PSI-697 2-(4-chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzohquinoline-4-carboxylic acid in vitro and in rodent models of vascular inflammation and thrombosis. J Pharmacol Exp Ther.2. 2. Myers DD Jr et al. Resolution of venous thrombosis using a novel oral small-molecule inhibitor of P-selecti

8、n (PSI-697) withoutanticoagulation. Thromb Haemost. 2007 Mar;97(3):400-7.3. 3. Myers DD Jr et al. Treatment with an oral small molecule inhibitor of P selectin (PSI-697) decreases vein wall injury in a rat stenosismodel of venous thrombosis. J Vasc Surg. 2006 Sep;44(3):625-32.McePdfHeightCaution: Product has not been fully validated for medical applications.