ASP-4058
目录号: PL06763 纯度: ≥99%
CAS No. :952565-91-2
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中文名称
ASP-4058
英文名称
ASP-4058
英文别名
ASP4058;01J7526K2Q;5-(5-(3-(Trifluoromethyl)-4-(((2S)-1,1,1-trifluoropropan-2-yl)oxy)phenyl)-1,2,4-oxadiazol-3-yl)-1H-benzimidazole;GTPL9569;DB11819;Q27231433;1H-Benzimidazole, 6-(5-(3-(trifluoromethyl)-4-((1S)-2,2,2-trifluoro-1-methylethoxy)phenyl)-1,2,4-oxadiazol-3-yl)-;3-(3H-benzimidazol-5-yl)-5-[3-(trifluoromethyl)-4-[(2S)-1,1,1-trifluoropropan-2-yl]oxyphenyl]-1,2;ASP-4058
Cas No.
952565-91-2
分子式
C19H12F6N4O2
分子量
442.31
包装储存
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
产品详情
ASP-4058 是一个选择性的、口服活性的鞘氨醇磷酸受体 1 和 5 (S1P1 and S1P5) 的二代激动剂,能改善小鼠实验性自身免疫性脑脊髓炎,具有良好的安全性。
生物活性
ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P 1 and S1P 5 ), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.
性状
Solid
IC50 & Target[1][2]
S1P1 and S1P5.
体内研究(In Vivo)
ASP4058 (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 vehicle-treated group is 15.5±0.619 in rats. ASP4058 prevents decreases in body weight of EAE rats.
ASP4058 (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 values for ASP4058 is 0.063 mg/kg. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
ClinicalTrial
参考文献
[1]. Rie Yamamoto, et al. ASP4058, a Novel Agonist for Sphingosine 1-Phosphate Receptors 1 and 5, Ameliorates Rodent Experimental Autoimmune Encephalomyelitis with a Favorable Safety Profile. PLoS One. 2014 Oct 27;9(10):e110819.
溶解度数据
In Vitro: DMSO : ≥ 50 mg/mL (113.04 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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