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- Pamoic acid disodium salt
Pamoic acid disodium salt
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.
| Physical Appearance | Pale yellow solid |
| Storage | Desiccate at RT |
| M.Wt | 432.33 |
| Cas No. | 6640-22-8 |
| Formula | C23H14Na2O6 |
| Solubility | insoluble in EtOH; ≥18 mg/mL in H2O; ≥28.6 mg/mL in DMSO |
| Chemical Name | sodium 1,1'-methylenebis(3-carboxynaphthalen-2-olate) |
| SDF | Download 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+] |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
U2OS cells expressing human GPR35a |
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Reaction Conditions |
15 min incubation |
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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] | |
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Animal models |
Male Swiss-Webster mice, 30–35 g |
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Dosage form |
25, 50 and 100 mg/kg Subcutaneous administration |
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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. |
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Note |
The technical data provided above is for reference only. |
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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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Quality Control & MSDS
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Chemical structure
