1. GPCR/G Protein
    Neuronal Signaling
  2. Orexin Receptor (OX Receptor)
  3. OX2R-IN-1

OX2R-IN-1 

Cat. No.: HY-149014
Handling Instructions

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.

For research use only. We do not sell to patients.

OX2R-IN-1 Chemical Structure

OX2R-IN-1 Chemical Structure

CAS No. : 2639148-08-4

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Description

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[1].

IC50 & Target

IC50: 484 μM (OX2R)

In Vitro

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 the BBB, since the PAMPA assay is limited by several drawbacks[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1].

Cell Line: CHO-K1 cell line
Concentration: 100-1000 µM
Incubation Time: 24h
Result: Exhibited low cytotoxic with IC50values of 484 μM
In Vivo

OX2R-IN-1 (compound 15) has a short half-life and poor bioavailability.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
Molecular Weight

457.97

Formula

C20H28ClN3O5S

CAS No.
SMILES

O=C(C1=CC=C(S(=O)(NC2=CC=CC(CN3CCC(CC3)CO)=C2)=O)N1C)OC.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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OX2R-IN-1
Cat. No.:
HY-149014
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