OX2R-IN-1

Modify Date: 2024-01-13 18:07:04

OX2R-IN-1 structure	Common Name	OX2R-IN-1
	CAS Number	2639148-08-4	Molecular Weight	457.97
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₀H₂₈ClN₃O₅S	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of OX2R-IN-1

OX2R-IN-1 is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 can cross the BBB into the brain with a short half-life[1].

Name	OX2R-IN-1

Description	OX2R-IN-1 is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 can cross the BBB into the brain with a short half-life[1].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Orexin Receptor (OX Receptor) Research Areas >> Neurological Disease
Target	IC50: 484 μM (OX2R)
In Vitro	OX2R-IN-1 (compound 15) has low cytotoxic withIC50 values of 484 μM. OX2R-IN-1 is significant and dose-dependently reduce the signal of orexin A-evoked response (0.2 μM) in CHO-K1 cell line. OX2R-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 IC50 values of 484 μM
In Vivo	OX2R-IN-1 has a short half-life and poor bioavailability. Animal Model: Albino male Wistar rats[1] 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: Parameter Units Plasma Brain tissuer t1/2,β (h)....... t1/2 min 9.63 14.85 tmax min 5 40 Cmax μmol/L 29.40 0.199 AUC μmol/L*min 1362.68 18.51 MRT min 39.94 68.93
References	[1]. Eva Mezeiova, et al. From orexin receptor agonist YNT-185 to novel antagonists with drug-like properties for the treatment of insomnia, Bioorg Chem. 2020 Oct;103:104179.

Molecular Formula	C₂₀H₂₈ClN₃O₅S
Molecular Weight	457.97