EST64454

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

EST64454 是一种高度可溶的 σ1 受体拮抗剂 (Ki : 22 nM)，具有治疗疼痛的潜力。

EST64454 is a highly soluble σ1 receptor antagonist (Ki : 22 nM),has the potential for?Pain Management.

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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.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. Animal Model:Male Wistar rats (250-300 g) Dosage:10 mg/kg Administration:P.o. (Pharmacokinetic Analysis) Result:The Cmax, t1/2, AUC0-∞, Vss and F% were 771 ng/mL, 3.4 hours, 1431 ng h/mL, 4.4 l/kg and 69%, respectively.

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Autophagy

Sigma receptor

σ1

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1950569-11-5

400.85

C18H23ClF2N4O2

>98% (HPLC)

In Vitro:?H2O : ≥ 100 mg/mL (249.47 mM))

CC(N1CCN(CCOCC2=NN(C3=CC=C(F)C(F)=C3)C=C2)CC1)=O.[H]Cl

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(-20℃)

With Ice Pack

≥ 2 years