TY-52156 - LPL Receptor Antagonist- MedChemExpress

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Inhibitors?Agonists?Screening Librarieswww.MedChemExpress.cnTY-52156Cat. No.:CAS No.:HY-19736934369-14-9C??H??Cl?N?O364.27LPL ReceptorGPCR/G ProteinPowder-20°C4°CIn solvent-80°C-20°C3 years2 years6 months1 month分?式:分?量:作?靶点:作?通路:储存?式:溶解性数据体外实验DMSO : ≥ 100 mg/mL (274.52 mM)H2O : < 0.1 mg/mL (insoluble)* \Mass1 mg2.7452 mL0.5490 mL0.2745 mL5 mg13.7261 mL2.7452 mL1.3726 mL10 mg27.4522 mL5.4904 mL2.7452 mLSolventConcentration制备储备液1 mM5 mM10 mM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?是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% saline Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution BIOLOGICAL ACTIVITY1/2

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?物活性IC50 & TargetTY-52156 是?种有效、选择性的 S1P3 受体拮抗剂，Ki 值为 110 nM [1]。Ki: 110 nM (S1P3) [1]TY-52156 inhibits the S1P3 receptor-dependent increase in [Ca2+]i [1]. TY-52156 shows submicromolar potency and a high degree of selectivity for S1P3 receptor [1]. TY-52156 (10 μM; 10 min) inhibits S1P-induced p44/p42 MAPK phosphorylation [1]. Western Blot Analysis [1]Cell Line:Concentration:Incubation Time:Result:Chinese hamster ovary K1 cells10 μM10 minInhibited S1P-induced p44/p42 MAPK phosphorylation.体外研究体内研究TY-52156 (10 mg/kg, 30 mg/kg; p.o.) suppresses S1P3 receptor-induced bradycardia after oral administration in vivo [1]. Animal Model:Dosage:Administration:Result:Male SD rats (290–340 g) [1]10 mg/kg, 30 mg/kgOral administrationInhibited S1P3 receptor-induced bradycardia after oral administration in vivo. 客户使?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 www.MedChemExpress.cn REFERENCES[1]. Murakami A, et al. Sphingosine 1-phosphate (S1P) regulates vascular contraction via S1P3 receptor: investigation based on a new S1P3 receptor antagonist. Mol Pharmacol. 2010 Apr;77(4):704-13.McePdfHeightCaution: Product has not been fully validated for medical applications. For research use only.

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