| Size | Price | Stock | Qty |
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| 100g |
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| 250g |
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| Other Sizes |
| Targets |
Pamoic acid disodium is a potent agonist of the orphan G protein-coupled receptor GPR35, with an EC₅₀ of 79 nM for GPR35 activation . The compound induces GPR35a internalization (EC₅₀ of 22 nM) and activates ERK1/2 signaling (EC₅₀ of 65 nM) . Additionally, pamoic acid disodium potently recruits β-arrestin2 to GPR35 .
EC50: 79 nM (GPR35), 65 nM (ERK1/2)[1] |
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| ln Vitro |
Pamoic acid (0.1 nM-0.1 mM) stimulates GPR35a internalization with an EC50 value of 22 nM[1]. Pamoic acid (0-10 μM) promotes ERK1/2 activation [1].
Pamoic acid disodium is a potent GPR35 agonist with an EC₅₀ of 79 nM . In U2OS cells, pamoic acid (0-10 μM) induces GPR35a internalization in a concentration-dependent manner with an EC₅₀ of 22 nM and activates ERK1/2 with an EC₅₀ of 65 nM . Western blot analysis shows concentration-dependent ERK1/2 activation with an EC₅₀ of 65 nM after 15 minutes of treatment at concentrations of 1, 10, 100 nM and 1, 10 μM . |
| ln Vivo |
In the abdominal contraction test, dose-related antinociceptive effects are induced by pamoic acid disodium (0-100 mg/kg; sc; once)[1].
In the abdominal constriction test using Swiss-Webster mice (30-35 g), pamoic acid disodium (0-100 mg/kg; s.c.; once) induces dose-related antinociception . The dose producing 50% antinociception (AD₅₀) is 40.5 mg/kg . The compound exhibits antinociceptive effects in a mouse model of visceral pain . |
| Cell Assay |
Western Blot Analysis[1]
Cell Types: U2OS cells Tested Concentrations: 1, 10, 100 nM and 1, 10 μM Incubation Duration: 15 min Experimental Results: A concentration-dependent activation of ERK1/2 was observed with an EC50 of 65 nM. Western Blot Analysis: U2OS cells are seeded in culture plates and treated with pamoic acid disodium at concentrations of 1, 10, 100 nM and 1, 10 μM for 15 minutes. After cell lysis, ERK1/2 phosphorylation levels are detected by Western blot, and the EC₅₀ for ERK1/2 activation is calculated as 65 nM . Internalization Assay: In cells expressing GPR35a, treatment with pamoic acid (0.1 nM-0.1 mM) for a defined period is followed by measuring the reduction in cell surface receptors to assess GPR35a internalization, with an EC₅₀ of 22 nM . β-arrestin2 Recruitment Assay: In cells co-expressing GPR35 and β-arrestin2, pamoic acid disodium treatment induces β-arrestin2 recruitment to GPR35 with an EC₅₀ of 79 nM . |
| Animal Protocol |
Animal/Disease Models: Swiss-Webster mice (30–35 g)[1]
Doses: 25, 50, and 100 mg/kg Route of Administration: subcutaneous (sc) injection, once Experimental Results: Elicited dose-related antinociception, the dose causing 50% antinociception being 40.5 mg /kg. Antinociceptive Assay (Abdominal Constriction Test): Swiss-Webster mice (30-35 g) are administered pamoic acid disodium subcutaneously at doses of 25, 50, or 100 mg/kg once. Abdominal constrictions are induced (e.g., using acetic acid), and the number of constrictions is counted to assess antinociceptive effects. The dose producing 50% antinociception (AD₅₀) is 40.5 mg/kg . Visceral Pain Model: The antinociceptive effects of pamoic acid disodium are evaluated in a mouse model of visceral pain . |
| References | |
| Additional Infomation |
Pamoic acid disodium (CAS: 6640-22-8) is a different compound from pamoic acid (CAS: 130-85-8); the former is the disodium salt form of the latter. As an important excipient, pamoic acid disodium plays a key role in the development of long-acting injectable formulations. Recent studies have revealed that pamoic acid itself possesses independent biological activity and can act as a potent agonist of GPR35. As a research tool compound, pamoic acid holds significant value in elucidating GPR35 pharmacology and in drug development aimed at stimulating GPR35.
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| Molecular Formula |
C23H14NA2O6
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|---|---|
| Molecular Weight |
432.33
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| Exact Mass |
432.058
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| CAS # |
6640-22-8
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| Related CAS # |
130-85-8 (Parent)
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| PubChem CID |
54676156
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| Appearance |
Off-white to light yellow solid powder
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| Boiling Point |
642.7ºC at 760 mmHg
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| Melting Point |
300 °C
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| Flash Point |
356.5ºC
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| LogP |
1.722
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
569
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C(=C1)C=C(C(=C2CC3=C(C(=CC4=CC=CC=C43)C(=O)O)[O-])[O-])C(=O)O.[Na+].[Na+]
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| InChi Key |
YGLLICRFEVEWOZ-UHFFFAOYSA-L
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| InChi Code |
InChI=1S/C23H16O6.2Na/c24-20-16(14-7-3-1-5-12(14)9-18(20)22(26)27)11-17-15-8-4-2-6-13(15)10-19(21(17)25)23(28)29;;/h1-10,24-25H,11H2,(H,26,27)(H,28,29);;/q;2*+1/p-2
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| Chemical Name |
disodium;3-carboxy-1-[(3-carboxy-2-oxidonaphthalen-1-yl)methyl]naphthalen-2-olate
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| Synonyms |
6640-22-8; Sodium pamoate; Disodium pamoate; RPO7LTE47E; NSC-49174;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (231.30 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 7.5 mg/mL (17.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 75.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 7.5 mg/mL (17.35 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 75.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3130 mL | 11.5652 mL | 23.1305 mL | |
| 5 mM | 0.4626 mL | 2.3130 mL | 4.6261 mL | |
| 10 mM | 0.2313 mL | 1.1565 mL | 2.3130 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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