OX2R-IN-1
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.
- CAS No.: 2639148-08-4
- Formula: C20H28ClN3O5S
- Molecular Weight:457.97
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Orexin Receptor (OX Receptor) Isoforms
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Biological Activity
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OX2 Receptor |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CHO-K1 cell line
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Concentration:100-1000 µM
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Incubation Time:24h
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Result:Exhibited low cytotoxic with IC50values of 484 μM
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Albino male Wistar rats[1]
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Dosage:75 mg/kg
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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
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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
Chemical Information
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CAS No. 2639148-08-4
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Molecular Weight 457.97
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Formula C20H28ClN3O5S
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SMILES
O=C(C1=CC=C(S(=O)(NC2=CC=CC(CN3CCC(CC3)CO)=C2)=O)N1C)OC.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)