TY-52156 - LPL Receptor Antagonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETY-52156Cat. No.: HY-19736CAS No.: 934369-14-9分式: CHClNO分量: 364.27作靶点: LPL Receptor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 : 100 mg/mL (274.52 mM)H2O : 40% PEG300 5

2、% Tween-80 45% salineSolubility: 2.5 mg/mL (6.86 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 TY-52156种有效、选择性的 S1P3 受体拮抗剂，Ki 值为 110 nM 1。IC50 & Target Ki: 110 nM (S1P3) 1体外研究 TY-52156 inhibits the S1P3 receptor-dependent increase in Ca2+i 1.TY-52156 show

3、s submicromolar potency and a high degree of selectivity for S1P3 receptor 1.TY-52156 (10 M; 10 min) inhibits S1P-induced p44/p42 MAPK phosphorylation 1.Western Blot Analysis 1Cell Line: Chinese hamster ovary K1 cellsConcentration: 10 MIncubation Time: 10 minResult: Inhibited S1P-induced p44/p42 MAP

4、K phosphorylation.体内研究 TY-52156 (10 mg/kg, 30 mg/kg; p.o.) suppresses S1P3 receptor-induced bradycardia after oraladministration in vivo 1.Animal Model: Male SD rats (290340 g) 1Dosage: 10 mg/kg, 30 mg/kgAdministration: Oral administrationResult: Inhibited S1P3 receptor-induced bradycardia after ora

5、l administration in vivo.户使本产品发表的科研献 EBioMedicine. 2019 Feb;40:210-223. Oncogene. 2017 Jun 29;36(26):3760-3771. Exp Ther Med. 2018 Jun;15(6):5007-5016.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Murakami A, et al. Sphingosine 1-phosphate (S1P) regulates vascular contraction via S1P3 receptor: investigation based on a newS1P3 receptor antagonist. Mol Pharmacol. 2010 Apr;77(4):704-13.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-379