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编 号:F754179
分子式:C20H28ClN3O5S
分子量:457.97
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生物活性:
OX2R-IN-1 (compound 15) is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 (compound 15) can cross the BBB into the brain with a short half-life.

体内研究:
OX2R-IN-1 (compound 15) has a short half-life and poor bioavailability.Animal Model:Albino male Wistar rats
Dosage:75 mg/kg
Administration:OX2R-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:ParameterUnits Plasma Brain tissuer
t1/2,β (h).......t1/2min9.6314.85
tmaxmin540
Cmaxμmol/L29.400.199
AUCμmol/L*min1362.6818.51
MRTmin39.9468.93


体外研究:
OX2R-IN-1 (compound 15) has low cytotoxic withIC50 values of 484 μM. OX2R-IN-1 (compound 15) is significant and dose-dependently reduce the signal of orexin A-evoked response (0.2 μM) in CHO-K1 cell line. OX2R-IN-1 (compound 15) has uncertain permeation through theBBB, since the PAMPA assay is limited by several drawbacks.
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