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。
货号:ajcx34744
CAS:1950569-11-5
分子式:C18H23ClF2N4O2
分子量：400.85
溶解度:DMSO : 100 mg/mL (249.47 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a Ki of 22 nM. EST64454 hydrochloride has the potential for the research of the pain[1].

EST64454 (10 mg/kg; p.o.; male Wistar rats) treatment shows the Cmax, t1/2, AUC0-∞, Vss and F% are 771 ng/mL, 3.4 hours, 1431 ng h/mL, 4.4 l/kg and 69%, respectively[1].EST64454 (10 mg/kg; p.o.; male CD1 mice) treatment shows the Cmax, t1/2, AUC0-∞, Vss and F% were 1178 ng/mL,<1 hours, 2645 ng h/mL, 1.2 l/kg and 60%, respectively[1].

[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.