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

Chemical Structure : Firazorexton

CAS No.: 2274802-95-6

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Firazorexton (TAK-994, TAK994)

货号: PC-38360Not For Human Use, Lab Use Only.

Firazorexton (TAK-994) is a potent, selective, orally available and brain-penetrant agonist of orexin 2 receptor (OX2R) with EC50 of 19 nM against recombinant human OX2R, 700-fold selectivity against OX1R.

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1 mg ￥2580 In stock
5 mg ￥4580 In stock
10 mg ￥7280 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Firazorexton (TAK-994) is a potent, selective, orally available and brain-penetrant agonist of orexin 2 receptor (OX2R) with EC50 of 19 nM against recombinant human OX2R, 700-fold selectivity against OX1R.
TAK-994 binds to hOX2R in a monophasic manner, with pKD of 7.07 and Bmax of 4.03 pmol/mg protein.
TAK-994 increased calcium mobilization in hOX2R/CHO-K1 cells in a dose-dependent manner with an EC50 value of 19 nM, with no effect on calcium mobilization using hOX1R/CHO-K1 cells.
TAK-994 dose-dependently increased IP1 contents with EC50 value of 16 nM in hOX2R/CHO-EA cell, increased β-arrestin recruitment with EC50 of 4.5 nM.
TAK-994 induced phosphorylation of ERK1/2 with EC50 of 19 nM and phosphorylation of CREB with EC50 of 2.9 nM nM, respectively, in hOX2R/CHO-EA cells.
TAK-994 (30 mg/kg, by mouth) significantly increased total wakefulness time in C57BL/6J mice, did not affect total wakefulness time in OX2R KO mice.

物理化学性质&存储条件

分子量 470.507
分子式 C22H25F3N2O4S
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,3S)-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. Takashi Ishikawa, et al. J Pharmacol Exp Ther. 2023 Jun;385(3):193-204.

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