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Pamoic acid disodium salt

双羟萘酸二钠, 乙炔酸二钠, 扑酸二钠盐
Catalog No.
B7638
GPR35激动剂
组合的产品项目
规格价格库存 数量
50mg
¥ 1,890.00
现货

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背景

Pamoic acid disodium salt, a supposedly inactive component in many formulations of drugs used to modulate release, is a potent agonist of the orphan receptor GPR35. GPR35 is a class A, rhodopsin-like G protein-coupled receptor (GPCR), strongly expressed in the lower intestine and colon, dorsal root ganglia, as well as a variety of immune cells including monocytes and dendritic cells. Targeting GPR35 provides potential therapeutic opportunities in a range of conditions, such as inflammation, pain and cancer.

References:

1. Zhao P, Sharir H, Kapur A, 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. Molecular Pharmacology, 2010, 78(4): 560-568.

2. Quon T, Lin LC, Ganguly A, et al. Therapeutic Opportunities and Challenges in Targeting the Orphan G Protein-Coupled Receptor GPR35. ACS Pharmacology & Translational Science, 2020, 3(5): 801-812.

文献引用

化学属性

Physical AppearancePale yellow solid
StorageDesiccate at RT
M.Wt432.33
Cas No.6640-22-8
FormulaC23H14Na2O6
Solubilityinsoluble in EtOH; ≥18 mg/mL in H2O; ≥28.6 mg/mL in DMSO
Chemical Namesodium 1,1'-methylenebis(3-carboxynaphthalen-2-olate)
SDFDownload SDF
Canonical SMILES[O-]C1=C(C2=CC=CC=C2C=C1C(O)=O)CC(C3=CC=CC=C3C=C4C(O)=O)=C4[O-].[Na+].[Na+]
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试验操作

Cell experiment:[1]

Cell lines

U2OS cells expressing human GPR35a

Reaction Conditions

15 min incubation

Applications

Pamoic acid potently recruited β-arrestin2 to GPR35 (EC50 = 79 nM), dose-dependently increased ERK1/2 phosphorylation (1 ~ 10 μM, 30 min incubation), and induced GPR35 translocation from the plasma membrane to the cytoplasm (EC50 = 22 nM) in U20S cells expressing human GPR35a.

Animal experiment:[1]

Animal models

Male Swiss-Webster mice, 30–35 g

Dosage form

25, 50 and 100 mg/kg

Subcutaneous administration

Applications

Pamoic acid exhibited dose-related antinociception in a mouse model of visceral pain perception, with an ED50 value of 40.5 mg/kg. Complete antinociception could be achieved with 100 mg/kg pamoic acid.

Note

The technical data provided above is for reference only.

References:

1. Zhao P, Sharir H, Kapur A, 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. Molecular Pharmacology, 2010, 78(4): 560-568.

2. Quon T, Lin LC, Ganguly A, et al. Therapeutic Opportunities and Challenges in Targeting the Orphan G Protein-Coupled Receptor GPR35. ACS Pharmacology & Translational Science, 2020, 3(5): 801-812.

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