2639148-08-4

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
Molecular Formula	C20H28ClN3O5S
Molecular Weight	457.97
MOL File	2639148-08-4.mol

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)

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Hazard Information

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
t_1/2,β (h)	t_1/2	min	9.63	14.85
t_max	min	5	40
C_max	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

Supplier

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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