TCS 3035GPR35 agonist CAS# 871085-49-3 |
- TC-G 1001
Catalog No.:BCC6316
CAS No.:494191-73-0
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| Cas No. | 871085-49-3 | SDF | Download SDF |
| PubChem ID | 2295463 | Appearance | Powder |
| Formula | C12H9NO5S | M.Wt | 279.27 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO | ||
| Chemical Name | 2-[4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]acetic acid | ||
| SMILES | C1=CC(=CC=C1C=C2C(=O)NC(=O)S2)OCC(=O)O | ||
| Standard InChIKey | WXMCOLGPDOYHNK-UITAMQMPSA-N | ||
| Standard InChI | InChI=1S/C12H9NO5S/c14-10(15)6-18-8-3-1-7(2-4-8)5-9-11(16)13-12(17)19-9/h1-5H,6H2,(H,14,15)(H,13,16,17)/b9-5- | ||
| 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 5.13 and 5.86 for rat and human GPR35 orthologs, respectively). |
TCS 3035 Dilution Calculator
TCS 3035 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.5808 mL | 17.9038 mL | 35.8076 mL | 71.6153 mL | 89.5191 mL |
| 5 mM | 0.7162 mL | 3.5808 mL | 7.1615 mL | 14.3231 mL | 17.9038 mL |
| 10 mM | 0.3581 mL | 1.7904 mL | 3.5808 mL | 7.1615 mL | 8.9519 mL |
| 50 mM | 0.0716 mL | 0.3581 mL | 0.7162 mL | 1.4323 mL | 1.7904 mL |
| 100 mM | 0.0358 mL | 0.179 mL | 0.3581 mL | 0.7162 mL | 0.8952 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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Target: GPR35
IC50: N/A
TCS3035, a GPR35 agonist, shows significantly high potency at rat and human GPR35 orthologs with pEC50 values of 5.13 and 5.86, respectively [1]. G protein-coupled receptors (GPCRs) are the largest and most studied group of transmembrane polypeptides. GPR35 is a poorly characterized G protein-coupled receptor that plays an important role in immune-modulation, gastric function and the regulation of insulin secretion. GPR35 is predominantly expressed in the gastro-intestinal tract and immune tissues. The tryptophan metabolite kynurenic acid has been suggested to be the endogenous ligand for GPR35 [1].
In vitro: Mutation to alanine of the conserved arginine at position 3.36 in either FLAG-hGPR35-eYFP or FLAG-rGPR35-eYFP resulted in a complete loss of agonist function of TCS3035 [1]. In addition, TCS3035-induced internalization of GPR35 is correlated with TCS3035 potency in receptor-β-arrestin-2 interaction BRET assays. Mutation to alanine of tyrosine 3.32 in transmembrane domain III abolished β-arrestin-2 recruitment in response to TCS3035 [1].
In vivo: N/A
Reference:
1. Jenkins L, Alvarez-Curto E, Campbell K, de Munnik S, Canals M, Schlyer S, et al. Agonist activation of the G protein-coupled receptor GPR35 involves transmembrane domain III and is transduced via Galpha(1)(3) and beta-arrestin-2. Br J Pharmacol. 2011;162(3):733-48.
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Agonist activation of the G protein-coupled receptor GPR35 involves transmembrane domain III and is transduced via Galpha(1)(3) and beta-arrestin-2.[Pubmed:20958291]
Br J Pharmacol. 2011 Feb;162(3):733-48.
BACKGROUND AND PURPOSE: GPR35 is a poorly characterized G protein-coupled receptor at which kynurenic acid has been suggested to be the endogenous ligand. We wished to test this and develop assays appropriate for the study of this receptor. EXPERIMENTAL APPROACH: Human and rat orthologues of GPR35 were engineered and expressed and assays developed to assess interaction with beta-arrestin-2, activation of Galpha(1)(3) and agonist-induced internalization. KEY RESULTS: GPR35-beta-arrestin-2 interaction assays confirmed that both the endogenous tryptophan metabolite kynurenic acid and the synthetic ligand zaprinast had agonist action at each orthologue. Zaprinast was substantially more potent than kynurenic acid at each and both agonists displayed substantially greater potency at rat GPR35. Two novel thiazolidinediones also displayed agonism and displayed similar potency at each GPR35 orthologue. The three ligand classes acted orthosterically with respect to each other, suggesting overlapping binding sites and, consistent with this, mutation to alanine of the conserved arginine at position 3.36 or tyrosine 3.32 in transmembrane domain III abolished beta-arrestin-2 recruitment in response to each ligand at each orthologue. CONCLUSIONS AND IMPLICATIONS: These studies indicate that beta-arrestin-2 interaction assays are highly appropriate to explore the pharmacology of GPR35 and that Galpha(1)(3) activation is an alternative avenue of signal generation from GPR35. Arginine and tyrosine residues in transmembrane domain III are integral to agonist recognition and function of this receptor. The potency of kynurenic acid at human GPR35 is sufficiently low, however, to question whether it is likely to be the true endogenous ligand for this receptor.
