A Gβγ-signaling-biased 5-OxoETE receptor antagonist; inhibits 5-OxoETE-induced neutrophil and eosinophil shape change and chemotaxis; inhibits 5-OxoETE-induced Gβγ-mediated IP1 production in HEK293 cells transiently expressing the 5-OxoETE receptor

Gue1654 – 25 mg

Brand:
Cayman
CAS:
397290-30-1
Storage:
-20
UN-No:
Non-Hazardous - /

Gue1654 is a Gβγ-signaling-biased 5-OxoETE receptor antagonist.{46628} It inhibits neutrophil and eosinophil shape change and chemotaxis induced by 5-OxoETE (Item No. 34250) but not chemoattractant C5a or prostaglandin D2 (PGD2; Item No. 12010). 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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SKU: 29686 - 25 mg Category:

Description

A Gβγ-signaling-biased 5-OxoETE receptor antagonist; inhibits 5-OxoETE-induced neutrophil and eosinophil shape change and chemotaxis; inhibits 5-OxoETE-induced Gβγ-mediated IP1 production in HEK293 cells transiently expressing the 5-OxoETE receptor, but has no effect on IP1 production induced by stimulation of endogenous Gαq-linked muscarinic receptors; in a BRET assay, reduces the 5-OxoETE-induced, but not basal, BRET fluorescence response

Formal name: N-[7-(methylthio)benzo[1,2-d:4,3-d′]bisthiazol-2-yl]-α-phenyl-benzeneacetamide

Synonyms: 

Molecular weight: 447.6

CAS: 397290-30-1

Purity: ≥95%

Formulation: A solid

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