TC-G 1001CAS# 494191-73-0 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 494191-73-0 | SDF | Download SDF |
| PubChem ID | 5766343 | Appearance | Powder |
| Formula | C17H11FN2O3S | M.Wt | 342.34 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 10 mM in DMSO | ||
| Chemical Name | 4-[(Z)-[2-(2-fluoroanilino)-4-oxo-1,3-thiazol-5-ylidene]methyl]benzoic acid | ||
| SMILES | C1=CC=C(C(=C1)NC2=NC(=O)C(=CC3=CC=C(C=C3)C(=O)O)S2)F | ||
| Standard InChIKey | SYCKPHBALHXMIR-ZROIWOOFSA-N | ||
| Standard InChI | InChI=1S/C17H11FN2O3S/c18-12-3-1-2-4-13(12)19-17-20-15(21)14(24-17)9-10-5-7-11(8-6-10)16(22)23/h1-9H,(H,22,23)(H,19,20,21)/b14-9- | ||
| 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. |
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| 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. |
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| 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 (pEC50 values are 7.59 and 8.36 for β-arrestin and Gαq-i5 Ca2+ assays respectively). Displays 1000-fold greater potency at human GPR35 receptors relative to mouse and rat GPR35 orthologs in an IP1 accumulation assay. More potent than zaprinast. |
TC-G 1001 Dilution Calculator
TC-G 1001 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.9211 mL | 14.6054 mL | 29.2107 mL | 58.4215 mL | 73.0268 mL |
| 5 mM | 0.5842 mL | 2.9211 mL | 5.8421 mL | 11.6843 mL | 14.6054 mL |
| 10 mM | 0.2921 mL | 1.4605 mL | 2.9211 mL | 5.8421 mL | 7.3027 mL |
| 50 mM | 0.0584 mL | 0.2921 mL | 0.5842 mL | 1.1684 mL | 1.4605 mL |
| 100 mM | 0.0292 mL | 0.1461 mL | 0.2921 mL | 0.5842 mL | 0.7303 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. | |||||
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High-throughput identification and characterization of novel, species-selective GPR35 agonists.[Pubmed:23262279]
J Pharmacol Exp Ther. 2013 Mar;344(3):568-78.
Drugs targeting the orphan receptor GPR35 have potential therapeutic application in a number of disease areas, including inflammation, metabolic disorders, nociception, and cardiovascular disease. Currently available surrogate GPR35 agonists identified from pharmacologically relevant compound libraries have limited utility due to the likelihood of off-target effects in vitro and in vivo and the variable potency that such ligands exhibit across species. We sought to identify and characterize novel GPR35 agonists to facilitate studies aimed at defining the physiologic role of GPR35. PathHunter beta-arrestin recruitment technology was validated as a human GPR35 screening assay, and a high-throughput screen of 100,000 diverse low molecular weight compounds was conducted. Confirmed GPR35 agonists from five distinct chemotypes were selected for detailed characterization using both beta-arrestin recruitment and G protein-dependent assays and each of the human, mouse, and rat GPR35 orthologs. These studies identified 4-{(Z)-[(2Z)-2-(2-fluorobenzylidene)-4-oxo-1,3-thiazolidin-5-ylidene]methyl}benzo ic acid (compound 1) as the highest potency full agonist of human GPR35 yet described. As with certain other GPR35 agonists, compound 1 was markedly selective for human GPR35, but displayed elements of signal bias between beta-arrestin-2 and G protein-dependent assays. Compound 1 also displayed competitive behavior when assessed against the human GPR35 antagonist, ML-145 (2-hydroxy-4-[4-(5Z)-5-[(E)-2-methyl-3-phenylprop-2-enylidene]-4-oxo-2-sulfanylid ene-1,3-thiazolidin-3-yl]butanoylamino]benzoic acid). Of the other chemotypes studied, compounds 2 and 3 were selective for the human receptor, but compounds 4 and 5 demonstrated similar activity at human, rat, and mouse GPR35 orthologs. Further characterization of these compounds and related analogs is likely to facilitate a better understanding of GPR35 in health and disease.
