*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
生物活性
Pamoic acid disodium is a potent GPR35 agonist with an EC50 value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect.
性状
Solid
IC50 & Target[1][2]
EC50: 79 nM (GPR35), 65 nM (ERK1/2)
体外研究(In Vitro)
Pamoic acid (0.1 nM-0.1 mM) induces GPR35a internalization with an EC50 value of 22 nM.
Pamoic acid (0-10 μM) induces ERK1/2 activation.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis
Cell Line: U2OS cells
Concentration: 1, 10, 100 nM and 1, 10 μM
Incubation Time: 15 min
Result: A concentration-dependent activation of ERK1/2 was observed with an EC50 of 65 nM.
体内研究(In Vivo)
Pamoic acid disodium (0-100 mg/kg; s.c.; once) induces a dose-related antinociception in the abdominal constriction test.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Swiss-Webster mice (30–35 g)
Dosage: 25, 50, and 100 mg/kg
Administration: Subcutaneous injection, once
Result: Elicited dose-related antinociception, the dose causing 50% antinociception being 40.5 mg/kg.
运输条件
Room temperature or refrigerated transportation.
储存方式
Sealed and stored at 4℃，, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Pingwei Zhao, et al. Targeting of the orphan receptor GPR35 by pamoic acid: a potent activator of extracellular signal-regulated kinase and β-arrestin2 with antinociceptive activity. Mol Pharmacol. 2010 Oct;78(4):560-8. [Information]
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