Gue 1654CAS# 397290-30-1 |
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Quality Control & MSDS
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| Cas No. | 397290-30-1 | SDF | Download SDF |
| PubChem ID | 5066134 | Appearance | Powder |
| Formula | C23H17N3OS3 | M.Wt | 447.6 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 50 mM in DMSO | ||
| Chemical Name | N-(2-methylsulfanyl-[1,3]thiazolo[4,5-g][1,3]benzothiazol-7-yl)-2,2-diphenylacetamide | ||
| SMILES | CSC1=NC2=C(S1)C3=C(C=C2)N=C(S3)NC(=O)C(C4=CC=CC=C4)C5=CC=CC=C5 | ||
| Standard InChIKey | UFOBDFMYJABXGK-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C23H17N3OS3/c1-28-23-25-17-13-12-16-19(20(17)30-23)29-22(24-16)26-21(27)18(14-8-4-2-5-9-14)15-10-6-3-7-11-15/h2-13,18H,1H3,(H,24,26,27) | ||
| 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 | Oxoeicosanoid receptor 1 (OXE-R) modulator. Selectively inhibits Gβγ but not Gαi signaling upon activation of the Gαi-βγ heterotrimer by OXE-R. Inhibits Gβγ-mediated opening of GIRK1/2 channels in HEK293 cells. |
Gue 1654 Dilution Calculator
Gue 1654 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2341 mL | 11.1707 mL | 22.3414 mL | 44.6828 mL | 55.8534 mL |
| 5 mM | 0.4468 mL | 2.2341 mL | 4.4683 mL | 8.9366 mL | 11.1707 mL |
| 10 mM | 0.2234 mL | 1.1171 mL | 2.2341 mL | 4.4683 mL | 5.5853 mL |
| 50 mM | 0.0447 mL | 0.2234 mL | 0.4468 mL | 0.8937 mL | 1.1171 mL |
| 100 mM | 0.0223 mL | 0.1117 mL | 0.2234 mL | 0.4468 mL | 0.5585 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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A biased ligand for OXE-R uncouples Galpha and Gbetagamma signaling within a heterotrimer.[Pubmed:22634634]
Nat Chem Biol. 2012 Jul;8(7):631-8.
Differential targeting of heterotrimeric G protein versus beta-arrestin signaling are emerging concepts in G protein-coupled receptor (GPCR) research and drug discovery, and biased engagement by GPCR ligands of either beta-arrestin or G protein pathways has been disclosed. Herein we report on a new mechanism of ligand bias to titrate the signaling specificity of a cell-surface GPCR. Using a combination of biomolecular and virtual screening, we identified the small-molecule modulator Gue1654, which inhibits Gbetagamma but not Galpha signaling triggered upon activation of Galpha(i)-betagamma by the chemoattractant receptor OXE-R in both recombinant and human primary cells. Gue1654 does not interfere nonspecifically with signaling directly at or downstream of Gbetagamma. This hitherto unappreciated mechanism of ligand bias at a GPCR highlights both a new paradigm for functional selectivity and a potentially new strategy to develop pathway-specific therapeutics.
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