2639148-08-4
2639148-08-4 structure
- Name: OX2R-IN-1
- Chemical Name: OX2R-IN-1
- CAS Number: 2639148-08-4
- Molecular Formula: C20H28ClN3O5S
- Molecular Weight: 457.97
- Catalog: Signaling Pathways GPCR/G Protein Orexin Receptor (OX Receptor)
- Create Date: 2022-08-13 21:34:08
- Modify Date: 2024-01-13 18:07:04
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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]. |
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| Related Catalog | |
| 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 |
| Molecular Formula | C20H28ClN3O5S |
|---|---|
| Molecular Weight | 457.97 |