Pamoic acid is a potent agonist of GPR35 orphan receptors (EC = 79 nM in a β-arrestin recruitment assay). It induces GPR35 translocation from the plasma membrane to the cytoplasm with an EC value of 22 nM. Pamoic acid also increases ERK1/2 phosphorylation in a concentration-dependent manner in U20S cells expressing human GPR35a. In vivo, pamoic acid has antinociceptive effects with an ED value of 40.5 mg/kg in a mouse abdominal constriction model of visceral pain perception. Pamoate salts, of which pamoic acid is the main constituent, have been used in drug formulations to extend the duration of action.
Pamoic acid (Embonic acid) is a potent GPR35 agonist with an EC50 of 79 nM. Pamoic acid exhibits neuroprotective and anti-inflammatory properties[1][2].
IC50&Target
EC50: 79 nM (GPR35)
体外研究
Pamoic acid activation of GPR35 may increase phosphorylation of ERK1/2, thereby initiating anti-inflammatory signaling by inhibiting NF - κ B-dependent inflammatory genes [1].
体内研究
In a mouse model of stroke, Pamoic acid (sc; 50-100 mg/kg) activates GPR35 and has neuroprotective effects. Pharmacological inhibition of GPR35 indicates that Pamoic acid reduces infarct size in a GPR35 dependent manner. Pamoic acid treatment leads to a preferential increase in non inflammatory Ly-6CLo monocytes/macrophages and a decrease in neutrophil count in ischemic brain [1].
分子式
C23H16O6
分子量
388.38
CAS号
130-85-8
中文名称
亚甲基双羟萘酸;帕莫酸
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
2-8°C, protect from light, stored under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro:
DMSO : 50 mg/mL (128.74 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
2.5748 mL
12.8740 mL
25.7480 mL
5 mM
0.5150 mL
2.5748 mL
5.1496 mL
10 mM
0.2575 mL
1.2874 mL
2.5748 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: