N8279 | GHSR1a agonist | Probechem Biochemicals

Chemical Structure : N8279

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N8279 (NCATS-SM8864)

货号: PC-72842Not For Human Use, Lab Use Only.

N8279 (NCATS-SM8864) is a selective, brain-penetrant small molecule Gαq-biased GHSR1a agonist with binding IC50 of 1.3 uM.

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生物&药学活性

N8279 (NCATS-SM8864) is a selective, brain-penetrant small molecule Gαq-biased GHSR1a agonist with binding IC50 of 1.3 uM.
N8279 is nearly an order of magnitude (8.9-fold) more potent than the endogenous ligand ghrelin and is a full agonist.
iCa2+ EC50 of N8279 is 41-fold more potent than its GHSR1a binding IC50, suggesting possible allosteric activity, which could be competitively inhibited by GHSR1a antagonists YIL781 and JMV2959.
N8279 is a weak activator of GHSR1a-mediated, βarr2-dependent cellular responses relative to ghrelin.
N8279 requires receptor sites and/or conformational states driven by the GHSR1a ECD that are distinct from ghrelin.
N8279 is brain-penetrant and attenuates aberrant DAergic behavior in mice.

物理化学性质&存储条件

分子量	472.922
分子式	C24H25ClN2O6
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	6-chloro-3-(3,4-dimethoxybenzoyl)-N-(3-(dimethylamino)propyl)-4-oxo-4H-chromene-2-carboxamide

参考文献

1. J D Gross, et al. Proc Natl Acad Sci U S A. 2022 Mar 8;119(10):e2112397119.

N8279 (NCATS-SM8864)

生物&药学活性

物理化学性质&存储条件

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N8279 (NCATS-SM8864)

生物&药学活性

物理化学性质&存储条件

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