SERT-IN-2_product_DataBase

Bioactivity

SERT-IN-2 is a potent SERT inhibitor (IC50=0.58 nM) with promising anti-depression efficacy. SERT-IN-2 shows good bioavailability of 83.28% in rats. SERT-IN-2 can cross the blood-brain barrier[1].

Target

IC50: 0.58 nM (SERT)

In Vivo

SERT-IN-2 (DH4) (2.5 mg/kg, 5 mg/kg; 口服或静脉注射; 单次剂量) 显示高血浆暴露和口服生物利用度在狗和大鼠[1]。SERT-IN-2 (10 mg/kg; 腹腔注射; 单次剂量) 可以穿过 SD 大鼠的血脑屏障[1]。SERT-IN-2 (1-10 mg/kg; 腹腔注射; 单次剂量) 抑制 5-羟色胺的摄取，并有效拮抗大鼠下丘脑中 p-chloroamphetamine (PCA) 诱导的 5-羟色胺的消耗[1]。SERT-IN-2 (1-10 mg/kg; 静脉注射; 试验前给药 3 次) 对大鼠有抗抑郁作用，并呈剂量依赖性地减少强迫游泳试验 (FST) 的不动次数[1]。药代动力学分析[1]

Name

SERT-IN-2

CAS

2055228-33-4

Formula

C26H24F2N6

Molar Mass

458.51

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Wang ZZ, et al. Deciphering Nonbioavailable Substructures Improves the Bioavailability of Antidepressants by Serotonin Transporter. J Med Chem. 2023 Jan 12;66(1):371-383.

PeptideDB

SERT-IN-2

CAS: 2055228-33-4 F: C26H24F2N6 W: 458.51