PN6047 | DOR agonist | Probechem Biochemicals

Chemical Structure : PN6047

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PN6047 (PN 6047)

货号: PC-49002Not For Human Use, Lab Use Only.

PN6047 is an orally bioavailable, G protein-biased and selective δ opioid agonist with pKi of 7.25, fully engages G protein signaling but is a partial agonist in both the arrestin recruitment and internalization assays.

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生物&药学活性

PN6047 is an orally bioavailable, G protein-biased and selective δ opioid agonist with pKi of 7.25, fully engages G protein signaling but is a partial agonist in both the arrestin recruitment and internalization assays.
PN6047 elicited a concentration-dependent activation of Gαi G proteins in cells expressing the human δ opioid receptor with EC50 of 13.5 nM, with no effect on Gαi activation in cells expressing either the rat µ opioid receptor or human κ opioid receptors.
PN6047 (1, 3, 10 mg/kg, p.o.) is an effective antihyperalgesic in the mouse MIA model of osteoarthritis but not in the carrageenan model of acute inflammatory pain.
PN6047 does not appear to have proconvulsive activity or induce analgesic tolerance.

物理化学性质&存储条件

分子量	460.596
分子式	C26H28N4O2S
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	3-[[4-(dimethylcarbamoyl)phenyl]-[1-(thiazol-5-ylmethyl)-4-piperidylidene]methyl]benzamide

参考文献

1. Alexandra E Conibear, et al. J Pharmacol Exp Ther. 2020 Feb;372(2):224-236.

PN6047 (PN 6047)

生物&药学活性

物理化学性质&存储条件

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PN6047 (PN 6047)

生物&药学活性

物理化学性质&存储条件

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