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)