Pamoic acid disodium saltGPR35 agonist CAS# 6640-22-8 |
- GDC-0068 (RG7440)
Catalog No.:BCC1271
CAS No.:1001264-89-6
- MK-2206 dihydrochloride
Catalog No.:BCC1274
CAS No.:1032350-13-2
- AZD5363
Catalog No.:BCC1073
CAS No.:1143532-39-1
- A-443654
Catalog No.:BCC1321
CAS No.:552325-16-3
- AKT inhibitor VIII
Catalog No.:BCC1334
CAS No.:612847-09-3
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 6640-22-8 | SDF | Download SDF |
PubChem ID | 16219861 | Appearance | Powder |
Formula | C23H14Na2O6 | M.Wt | 432.33 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | Soluble to 100 mM in water and to 75 mM in DMSO | ||
Chemical Name | 4-[(3-carboxy-2-hydroxynaphthalen-1-yl)methyl]-3-hydroxynaphthalene-2-carboxylic acid;sodium | ||
SMILES | C1=CC=C2C(=C1)C=C(C(=C2CC3=C(C(=CC4=CC=CC=C43)C(=O)O)O)O)C(=O)O.[Na] | ||
Standard InChIKey | MQIPLTYHZCWJRA-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C23H16O6.Na/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); | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | GPR35 agonist. Induces GPR35 internalization and activates ERK1/2 (EC50 values are 22 and 65 nM respectively). Mediates recruitment of β-arrestin2 to GPR35. Also exhibits antinociceptive effects in a mouse model of visceral pain. |
Pamoic acid disodium salt Dilution Calculator
Pamoic acid disodium salt Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.313 mL | 11.5652 mL | 23.1305 mL | 46.261 mL | 57.8262 mL |
5 mM | 0.4626 mL | 2.313 mL | 4.6261 mL | 9.2522 mL | 11.5652 mL |
10 mM | 0.2313 mL | 1.1565 mL | 2.313 mL | 4.6261 mL | 5.7826 mL |
50 mM | 0.0463 mL | 0.2313 mL | 0.4626 mL | 0.9252 mL | 1.1565 mL |
100 mM | 0.0231 mL | 0.1157 mL | 0.2313 mL | 0.4626 mL | 0.5783 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
- 5alpha-Hydroxychloranthalactone A
Catalog No.:BCN7469
CAS No.:66395-04-8
- Chloranthalactone B
Catalog No.:BCN8020
CAS No.:66395-03-7
- Chloranthalactone A
Catalog No.:BCN8022
CAS No.:66395-02-6
- (+)-Apogossypol
Catalog No.:BCC5585
CAS No.:66389-74-0
- Methylsyringol
Catalog No.:BCN3535
CAS No.:6638-05-7
- TGX-221
Catalog No.:BCC1244
CAS No.:663619-89-4
- Ranitidine Hydrochloride
Catalog No.:BCC4533
CAS No.:66357-59-3
- Ranitidine
Catalog No.:BCC9134
CAS No.:66357-35-5
- 5'-Deoxy-5-fluorocytidine
Catalog No.:BCC8746
CAS No.:66335-38-4
- Dihydroguaiaretic acid
Catalog No.:BCN4212
CAS No.:66322-34-7
- ML 171
Catalog No.:BCC6252
CAS No.:6631-94-3
- 3H-1,2-Benzodithiol-3-one-1,1-dioxide
Catalog No.:BCC8633
CAS No.:66304-01-6
- 13-Hydroxyoxyberberine
Catalog No.:BCN3355
CAS No.:66408-27-3
- 6-Amino-1,3-dimethyluracil
Catalog No.:BCC8755
CAS No.:6642-31-5
- 2-(2,4-Diaminophenoxy)ethanol dihydrochloride
Catalog No.:BCN8497
CAS No.:66422-95-5
- Kaempferol 3-O-(6''-O-acetyl)glucoside-7-O-rhamnoside
Catalog No.:BCN1385
CAS No.:66465-24-5
- H-D-Lys(Boc)-OMe.HCl
Catalog No.:BCC2990
CAS No.:66494-53-9
- JW 55
Catalog No.:BCC2453
CAS No.:664993-53-7
- Amantadine HCl
Catalog No.:BCC4465
CAS No.:665-66-7
- Bicifadine hydrochloride
Catalog No.:BCC7925
CAS No.:66504-75-4
- MSOP
Catalog No.:BCC6801
CAS No.:66515-29-5
- Benzoin isopropyl ether
Catalog No.:BCC8856
CAS No.:6652-28-4
- Propacetamol hydrochloride
Catalog No.:BCC9129
CAS No.:66532-86-3
- Ansamitocin P-3
Catalog No.:BCN8373
CAS No.:66547-09-9
Antagonists of GPR35 display high species ortholog selectivity and varying modes of action.[Pubmed:22967846]
J Pharmacol Exp Ther. 2012 Dec;343(3):683-95.
Variation in pharmacology and function of ligands at species orthologs can be a confounding feature in understanding the biology and role of poorly characterized receptors. Substantial selectivity in potency of a number of GPR35 agonists has previously been demonstrated between human and rat orthologs of this G protein-coupled receptor. Via a bioluminescence resonance energy transfer-based assay of induced interactions between GPR35 and beta-arrestin-2, addition of the mouse ortholog to such studies indicated that, as for the rat ortholog, murine GPR35 displayed very low potency for pamoate, whereas potency for the reference GPR35 agonist zaprinast was intermediate between the rat and human orthologs. This pattern was replicated in receptor internalization and G protein activation assays. The effectiveness and mode of action of two recently reported GPR35 antagonists, methyl-5-[(tert-butylcarbamothioylhydrazinylidene)methyl]-1-(2,4-difluorophenyl)p yrazole-4-carboxylate (CID-2745687) and 2-hydroxy-4-[4-(5Z)-5-[(E)-2-methyl-3-phenylprop-2-enylidene]-4-oxo-2-sulfanylide ne-1,3-thiazolidin-3-yl]butanoylamino)benzoic acid (ML-145), were investigated. Both CID-2745687 and ML-145 competitively inhibited the effects at human GPR35 of cromolyn disodium and zaprinast, two agonists that share an overlapping binding site. By contrast, although ML-145 also competitively antagonized the effects of pamoate, CID-2745687 acted in a noncompetitive fashion. Neither ML-145 nor CID-2745687 was able to effectively antagonize the agonist effects of either zaprinast or cromolyn disodium at either rodent ortholog of GPR35. These studies demonstrate that marked species selectivity of ligands at GPR35 is not restricted to agonists and considerable care is required to select appropriate ligands to explore the function of GPR35 in nonhuman cells and tissues.
Targeting of the orphan receptor GPR35 by pamoic acid: a potent activator of extracellular signal-regulated kinase and beta-arrestin2 with antinociceptive activity.[Pubmed:20826425]
Mol Pharmacol. 2010 Oct;78(4):560-8.
Known agonists of the orphan receptor GPR35 are kynurenic acid, zaprinast, 5-nitro-2-(3-phenylproplyamino) benzoic acid, and lysophosphatidic acids. Their relatively low affinities for GPR35 and prominent off-target effects at other pathways, however, diminish their utility for understanding GPR35 signaling and for identifying potential therapeutic uses of GPR35. In a screen of the Prestwick Library of drugs and drug-like compounds, we have found that pamoic acid is a potent GPR35 agonist. Pamoic acid is considered by the Food and Drug Administration as an inactive compound that enables long-acting formulations of numerous drugs, such as the antihelminthics oxantel pamoate and pyrantel pamoate; the psychoactive compounds hydroxyzine pamoate (Vistaril) and imipramine pamoate (Tofranil-PM); and the peptide hormones triptorelin pamoate (Trelstar) and octreotide pamoate (OncoLar). We have found that pamoic acid induces a G(i/o)-linked, GPR35-mediated increase in the phosphorylation of extracellular signal-regulated kinase 1/2, recruitment of beta-arrestin2 to GPR35, and internalization of GPR35. In mice, it attenuates visceral pain perception, indicating an antinociceptive effect, possibly through GPR35 receptors. We have also identified in collaboration with the Sanford-Burnham Institute Molecular Libraries Probe Production Center new classes of GPR35 antagonist compounds, including the nanomolar potency antagonist methyl-5-[(tert-butylcarbamothioylhydrazinylidene)methyl]-1-(2,4-difluorophenyl)p yrazole-4-carboxylate (CID2745687). Pamoic acid and potent antagonists such as CID2745687 present novel opportunities for expanding the chemical space of GPR35, elucidating GPR35 pharmacology, and stimulating GPR35-associated drug development. Our results indicate that the unexpected biological functions of pamoic acid may yield potential new uses for a common drug constituent.