| Identification | Back Directory | [Name]
1H-Pyrrole-2-carboxylic acid, 5-[[[3-[[4-(hydroxymethyl)-1-piperidinyl]methyl]phenyl]amino]sulfonyl]-1-methyl-, methyl ester, hydrochloride (1:1) | [CAS]
2639148-08-4 | [Synonyms]
OX2R-IN-1
1H-Pyrrole-2-carboxylic acid, 5-[[[3-[[4-(hydroxymethyl)-1-piperidinyl]methyl]phenyl]amino]sulfonyl]-1-methyl-, methyl ester, hydrochloride (1:1) | [Molecular Formula]
C20H28ClN3O5S | [MOL File]
2639148-08-4.mol | [Molecular Weight]
457.97 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
OX2R-IN-1 (compound 15) 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 |
|
| [IC 50]
OX2 Receptor | [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. DOI:10.1016/j.bioorg.2020.104179 |
|
|