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Merck
CN

370681

OXE-R-G βγ Coupling Modulator, Gue1654 - Calbiochem

别名:

7-(Methylthio)-2-((2,2-diphenylacetyl)amino)benzo[1,2-d:4,3-dʹ]bisthiazole, N-(7-(Methylsulfanyl)[1,3]thiazolo[4,5-g][1,3]benzothiazol-2-yl)-2,2-diphenylacetamide

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assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

color

tan

solubility

DMSO: 25 mg/mL

General description

A membrane-permeant amidobenzobisthiazolo compound that modulates OXE-R-Gβγ coupling upon receptor stimulation via direct OXE-R interaction, but not preexisting OXE-R-Gαβ interaction. Shown to selectively inhibit OXE-R-Gβγ coupling-mediated, but not OXE-R-Gα-mediated, downstream signalings in HEK293 as well as primary human eosinophils and neutrophils (Effective Conc. 1 to 30 μM), displaying no inhibitory activity against cellular functions mediated by Gα or Gβγ when coupled to other GPCRs, including PGD2 receptor CRTH2 (DP2), IL8 receptors CXCR1/2, muscarinic receptor, and C5a receptor. Comparing to Gallein (Cat. No. 371708), Gue1654 does not exert its activity via direct Gβγ interaction.
A membrane-permeant amidobenzobisthiazolo compound that modulates OXE-R-Gβγ coupling upon receptor stimulation via direct OXE-R interaction, without affecting preexisting OXE-R-Gαβ interaction. Selectively inhibits OXE-R-Gβγ coupling-mediated, but not OXE-R-Gα-mediated, downstream cellular signalings (Effective Conc. 1 to 30 μM), displaying no inhibitory activity against cellular functions mediated by Gα or Gβγ when coupled to other GPCRs. Comparing to Gallein (Cat. No. 371708), Gue1654 does not exert its activity via direct Gβγ interaction.

Biochem/physiol Actions

OXE-R-Gβγ coupling

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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Stefanie Blättermann et al.
Nature chemical biology, 8(7), 631-638 (2012-05-29)
Differential targeting of heterotrimeric G protein versus β-arrestin signaling are emerging concepts in G protein-coupled receptor (GPCR) research and drug discovery, and biased engagement by GPCR ligands of either β-arrestin or G protein pathways has been disclosed. Herein we report

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