Chemical Property of N-(2-methylsulfanyl-[1,3]thiazolo[4,5-g][1,3]benzothiazol-7-yl)-2,2-di(phenyl)acetamide
Chemical Property:
- Storage Temp.:2-8°C
- Solubility.:DMSO: soluble5mg/mL (clear solution; warmed)
- XLogP3:6.5
- Hydrogen Bond Donor Count:1
- Hydrogen Bond Acceptor Count:6
- Rotatable Bond Count:5
- Exact Mass:447.05337569
- Heavy Atom Count:30
- Complexity:578
- Purity/Quality:
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≥97% by HPLC *data from raw suppliers
Gue 1654 *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:Xn
- Statements:
22
- MSDS Files:
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Useful:
- Canonical SMILES:CSC1=NC2=C(S1)C3=C(C=C2)N=C(S3)NC(=O)C(C4=CC=CC=C4)C5=CC=CC=C5
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Description
Gue1654 is a Gβγ-signaling-biased 5-OxoETE receptor antagonist. It inhibits neutrophil and eosinophil shape change and chemotaxis induced by 5-OxoETE (Item No. 34250) but not chemoattractant C5a or prostaglandin D2 (PGD2; ). Gue1654 inhibits 5-OxoETE-induced Gβγ-mediated inositol monophosphate (IP1) production in HEK293 cells transiently expressing the 5-OxoETE receptor, an effect that can be blocked by the Gβγ-inhibitor gallein, but has no effect on IP1 production induced by stimulation of endogenous Gαq-linked muscarinic receptors. In a bioluminescence resonance energy transfer (BRET) assay, Gue1654 reduces the 5-OxoETE-induced, but not basal, BRET fluorescence response, indicating disruption of the interaction between ligand-activated 5-OxoETE receptor and Gβγ.
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Uses
Gue 1654 is a selective inhibitor of OXE-R Gβγ signaling.
