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首页-小分子抑制剂&激动剂-GPCR-Orexin Receptor-IDOR-1117-1680
IDOR-1117-1680

Chemical Structure : IDOR-1117-1680

CAS No.: 3008559-42-7

IDOR-1117-1680 (DORA 31)

货号: PC-24473Not For Human Use, Lab Use Only.

IDOR-1117-1680 is a potent, dual orexin receptor antagonist with IC50 of 19 nM and 1.9 nM for hOX1R and hOX2R, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

IDOR-1117-1680 is a potent, dual orexin receptor antagonist with IC50 of 19 nM and 1.9 nM for hOX1R and hOX2R, respectively.
IDOR-1117-1680 displays exquisite binding constants on hOX2R (FLIPR Schild plot) with Kb values of 0.45 nM.
IDOR-1117-1680 does not show significant P450 inhibition (3A4T IC50 = 19 μM (T testosterone used as marker); 3A4M IC50 = 6.9 μM (M midazolam used as marker); 2C9 IC50 = 17 μM; 2D6 IC50 = >50 μM).
IDOR-1117-1680 effectively induced sleep in dogs.

物理化学性质&存储条件

分子量 438.93
分子式 C21H19ClN6OS
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

(5-Chloro-2-(2H-1,2,3-triazol-2-yl)phenyl)(2-((2-methylbenzo[d]thiazol-6-yl)methyl)pyrazolidin-1-yl)methanone

参考文献

1. Surivet JP, et al. Bioorg Med Chem. 2025 May 1;122:118132.

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