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首页-小分子抑制剂&激动剂-GPCR-Orexin Receptor-OX-201
OX-201

Chemical Structure : OX-201

CAS No.: 2460722-03-4

OX-201 (OX201)

货号: PC-22566Not For Human Use, Lab Use Only.

OX-201 is a potent, selective, BBB-penetrable orexin receptor 2 (OX2R) agonist with EC50 of 8.0 nM in calcium mobilization assay in hOX2R/CHO-K1 cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

OX-201 is a potent, selective, BBB-penetrable orexin receptor 2 (OX2R) agonist with EC50 of 8.0 nM in calcium mobilization assay in hOX2R/CHO-K1 cells.
OX-201 displays 1000-fold selectivity for OX2R over OX1R.
OX-201 at 10 μM does not show >50% inhibition or stimulation for 102 tested enzymes, receptors, or ion channels, except cannabinoid CB1 receptor (51% inhibition) and progesterone receptor B (53% inhibition).
OX-201 produced wake-promoting effects via OX2R activation in mice and rats.
OX-201 activated inspiratory neurons in the pre-Bötzinger complex in rat medullary slices.
OX-201 increased burst activity in rat isolated brainstem−spinal cord preparations.
OX-201 (3 mg/kg, i.v.) significantly increased burst frequency of the diaphragm in anesthetized rats.

物理化学性质&存储条件

分子量 506.49
分子式 C22H23F5N2O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-((2S,3R)-4,4-difluoro-1-(2-hydroxy-2-methylpropanoyl)-2-((2,3',5'-trifluoro-[1,1'-biphenyl]-3-yl)methyl)pyrrolidin-3-yl)methanesulfonamide

参考文献

1. Yamada R, et al. PLoS One. 2024 Jun 25;19(6):e0306099.

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