PZM21 | MOR agonist | Probechem Biochemicals

Chemical Structure : PZM21

CAS No.: 1997387-43-5

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PZM21 (PZM 21, PZM-21)

货号: PC-42356Not For Human Use, Lab Use Only.

PZM21 is a potent, selective Gi-biased μ-opioid-receptor (μOR, MOR) agonist with Ki/EC50 of 1.1/4.6 nM, has little to no detectable κOR/δOR agonist or nociceptin receptor agonist activity.

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生物&药学活性

PZM21 is a potent, selective Gi-biased μ-opioid-receptor (μOR, MOR) agonist with Ki/EC50 of 1.1/4.6 nM, has little to no detectable κOR/δOR agonist or nociceptin receptor agonist activity.
PZM21 is actually an κOR antagonist (Ki=18 nM), 500- to 1,000-fold weaker activity for hERG and neurotransmitter transporters; also has no detectable β-arrestin-2 recruitment in the PathHunter assay.
Unlike morphine, PZM21 is more efficacious for the affective component of analgesia versus the reflexive component and is devoid of both respiratory depression and morphine-like reinforcing activity in mice.

物理化学性质&存储条件

分子量	361.50158
分子式	C19H27N3O2S
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	Urea, N-[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-N'-[(1S)-1-methyl-2-(3-thienyl)ethyl]-

参考文献

1. Manglik A, et al. Nature. 2016 Sep 8;537(7619):185-190.

2. Kostic M. Cell Chem Biol. 2016 Sep 22;23(9):1039-1040.

PZM21 (PZM 21, PZM-21)

生物&药学活性

物理化学性质&存储条件

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PZM21 (PZM 21, PZM-21)

生物&药学活性

物理化学性质&存储条件

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