OX2R-IN-1是一种OX2R拮抗剂(一种潜在的OX2R结合剂) ，具有低细胞毒性，IC50值为484 μM。OX2R-IN-1可穿过血脑屏障，药物半衰期短。

OX 2 R-IN-1 is a low cytotoxicity profile OX 2 R-IN-1 antagonist (a potential OX2R binder) with an IC 50 value of 484 μM. OX 2 R-IN-1 can cross the BBB into the brain with a short half-life [1].

OX 2 R-IN-1 (compound 15) has low cytotoxic with IC 50 values of 484 μM. OX 2 R-IN-1 is significant and dose-dependently reduce the signal of orexin A-evoked response (0.2 μM) in CHO-K1 cell line. OX 2 R-IN-1 has uncertain permeation through the BBB, since the PAMPA assay is limited by several drawbacks [1]. Cell Cytotoxicity Assay [1]. Cell Line: CHO-K1 cell line Concentration: 100-1000 μM Incubation Time: 24h Result: Exhibited low cytotoxic with IC 50 values of 484 μM

OX 2 R-IN-1 has a short half-life and poor bioavailability. Animal Model: Albino male Wistar rats [1] Dosage: 75 mg/kg Administration: OX 2 R-IN-1 (75 mg/kg; intraperitoneal injection) blood samples are collected at 0, 5, 10, 20, 30, 40, 60, 90, 120 and 240 min with a short half-life and poor bioavailability Result: Parameter Units Plasma Brain tissuer t 1/2,β (h)....... t 1/2 min 9.63 14.85 t max min 5 40 C max μmol/L 29.40 0.199 AUC μmol/L*min 1362.68 18.51 MRT min 39.94 68.93

2639148-08-4

C20H28ClN3O5S

457.97

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years