EST64454 hydrochloride
目录号: PL11273 纯度: ≥99%
CAS No. :1950569-11-5
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中文名称
EST64454 hydrochloride
英文名称
EST64454 hydrochloride
英文别名
EST64454 hydrochloride;EST64454;EST64454 HCl;EST64454 (hydrochloride);1-[4-[2-[[1-(3,4-difluorophenyl)pyrazol-3-yl]methoxy]ethyl]piperazin-1-yl]ethanone;hydrochloride;BDBM50555105
Cas No.
1950569-11-5
分子式
C18H23ClF2N4O2
分子量
400.85
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
EST64454 hydrochloride 是一种选择性且具有口服活性的 sigma-1 受体拮抗剂,Ki 为 22 nM。EST64454 hydrochloride 具有研究疼痛的潜力。
生物活性
EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a K i of 22 nM. EST64454 hydrochloride has the potential for the research of the pain.
性状
Solid
体内研究(In Vivo)
EST64454 (10 mg/kg; p.o.; male Wistar rats) treatment shows the C max , t 1/2 , AUC 0-∞ , V ss and F% are 771 ng/mL, 3.4 hours, 1431 ng h/mL, 4.4 l/kg and 69%, respectively.
EST64454 (10 mg/kg; p.o.; male CD1 mice) treatment shows the C max , t 1/2 , AUC 0-∞ , V ss and F% were 1178 ng/mL, <1 hours, 2645 ng h/mL, 1.2 l/kg and 60%, respectively. 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, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Díaz JL, et al. EST64454: a Highly Soluble σ1 Receptor Antagonist Clinical Candidate for Pain Management. J Med Chem. 2020;63(23):14979-14988.
溶解度数据
In Vitro: H2O : ≥ 100 mg/mL (249.47 mM)DMSO : 100 mg/mL (249.47 mM; Need ultrasonic)
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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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