化合物ASP-4058 T10385

Product Introduction
Bioactivity


英文名: ASP-4058

描述: ASP-4058 是一种鞘氨醇磷酸受体 1 和 5 (S1P1 and S1P5) 的二代激动剂，具有选择性、安全性和口服活性。ASP-4058能改善小鼠实验性自身免疫性脑脊髓炎。

体外活性: ASP4058 (100 nM) significantly reduced FITC-dextran leakage through an endothelial monolayer and suppressed the migration of macrophages across the monolayer in vitro by using a Transwell system.[2]

体内活性: ASP4058 (0.1 and 0.3 mg/kg; p.o.; daily for day 12 to day 45) maintains the clinical score at a relatively low level and the cumulative clinical scores (18-45 dpi) among the groups treated with 0.1 and 0.3 mg/kg dosages are 6.90±2.85 and 5.60±2.21, respectively in mice. The ED50 value for ASP4058 is 0.063 mg/kg.[1]ASP4058 (0.03, 0.1, and 0.3 mg/kg; p.o., daily for 21 days) reduces the clinical score in a dose-dependent manner and the cumulative clinical score from day 0 to 21 dpi at 0.03, 0.1, and 0.3 mg/kg are 15.5±1.48, 9.50±2.17 and 1.17±1.17, respectively, while that of the vehicle-treated group is 15.5±0.619 in rats.[1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45.0 mg/mL (101.7 mM)


关键字: ASP-4058 | ASP4058 | ASP 4058

相关产品: PF-543 Citrate | PF-543 hydrochloride | Ponesimod | SK1-IN-1 | SKI-178 | MP-A08 | LX-2931 | SLP9101555 | CS 2100 | CYM-5541

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途