UCSF7447 | MT-1 inverse agonist | Probechem Biochemicals

Chemical Structure : UCSF7447

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UCSF7447 (UCSF-7447, ZINC555417447)

货号: PC-38133Not For Human Use, Lab Use Only.

UCSF7447 (UCSF-7447, ZINC555417447) is a potent, selecive, brain permeable melatonin receptor MT-1 inverse agonist with Ki of 304 nM (hMT-1).

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生物&药学活性

UCSF7447 (UCSF-7447, ZINC555417447) is a potent, selecive, brain permeable melatonin receptor MT-1 inverse agonist with Ki of 304 nM (hMT-1).
UCSF7447 increased basal cAMP with EC50 value of 41 nM at hMT1, selectivity for hMT1 over hMT2 of 53-fold, and hMT1 inverse agonist efficacies of 62%.
UCSF7447 advanced the onset of activity by approximately 1 hour at 0.9 μg/mouse (about 0.03 mg/Kg), an effect similar to that of melatonin at its ED50 (0.72 μg/mouse).
At a higher dose (30 μg/mouse, about 1 mg/Kg), UCSF7447 advanced the onset of running wheel activity with an amplitude similar to melatonin.

物理化学性质&存储条件

分子量	363.643
分子式	C15H12BrClN4
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	2-Bromo-4-chloro-N-[3-(1H-1,2,4-triazol-5-yl)phenyl]-benzenemethanamine

参考文献

1. Reed M Stein, et al. Nature. 2020 Mar;579(7800):609-614.

UCSF7447 (UCSF-7447, ZINC555417447)

生物&药学活性

物理化学性质&存储条件

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UCSF7447 (UCSF-7447, ZINC555417447)

生物&药学活性

物理化学性质&存储条件

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