Gue1654 | OXE-R biased antagonist

CAS:
 397290-30-1
Catalog Number:
 10-1425
GUE1654 chemical structure Focus Biomolecules

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5 mg$60.00
25 mg$240.00

Gue1654 (397290-30-1) is a biased antagonist for the oxoeicosanoid receptor 1 (OXE-R, GPR170)1, the receptor for 5-Oxo-ETE, a proinflammatory eicosanoid2. It selectively inhibits Gβγ but not Gαi signaling upon activation of the Gαi-βγ heterotrimer by OXE-R.1,3 Gue1654 alleviated coronary artery ligation-induced ischemic myocardial injury in a mouse model.4

References/Citations:

  1. Blatermann et al. (2012), A biased ligand for OXE-R uncouples Gα and Gßγ signaling within a heterotrimer; Nat. Chem. Biol., 8 631
  2. Powell and Rokach (2013), The eosinophil chemoattractant 5-oxo-ETE and the OXE receptor; Prog. Lipid Res., 52 651
  3. Konya et al. (2014), A biased non-Gαi OXE-R antagonist demonstrates that Gαi protein subunit is not directly involved in neutrophil, eosinophil, and monocyte activation by 5-oxo-ETE; J. Immunol., 192 4774
  4. Lai et al. (2021), Oxoeicosanoid receptor inhibition alleviates acute myocardial infarction though activation of BCAT1; Basic Res. Cardiol., 116 3
CAS:
397290-30-1
Catalog Number:
10-1425
Activity:
Biased OXE-R antagonist
Chemical Names:
N-[7-(Methylthio)benzo[1,2-d:4,3-d']bisthiazol-2-yl]-α-phenylbenzeneacetamide
Molecular Weight:
447.59
Molecular Formula:

C23H17N3OS3

Solubility:
Soluble in DMSO (40 mg/ml with warming)
Physical Properties:
Off-white solid
Purity:

>98% TLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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