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- TC-G 1001
TCS 3035GPR35 agonist |
Sample solution is provided at 25 µL, 10mM.
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Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
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TCS 3035 Dilution Calculator
calculate
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TCS 3035 Molarity Calculator
calculate
Cas No. | 871085-49-3 | SDF | Download SDF |
Chemical Name | (Z)-2-(4-((2,4-dioxothiazolidin-5-ylidene)methyl)phenoxy)acetic acid | ||
Canonical SMILES | O=C(/C(S1)=C/C2=CC=C(OCC(O)=O)C=C2)NC1=O | ||
Formula | C12H9NO5S | M.Wt | 279.27 |
Solubility | <27.93mg l="" in="" dmso="">27.93mg> | Storage | Store at -20°C |
Physical Appearance | Off White solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
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. |
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.