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GPR4 antagonist 3b

Chemical Structure : GPR4 antagonist 3b

CAS No.: 1883333-94-5

GPR4 antagonist 3b

Catalog No.: PC-61082Not For Human Use, Lab Use Only.

GPR4 antagonist 3b is the first potent and selective proton-sensing GPCR GPR4 antagonist with IC50 of 67 nM, with no activity against TDAG8 and OGR1 (IC50>10 uM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GPR4 antagonist 3b is the first potent and selective proton-sensing GPCR GPR4 antagonist with IC50 of 67 nM, with no activity against TDAG8 and OGR1 (IC50>10 uM).
GPR4 antagonist 3b effectively prolongs life in the mouse myocardial infarction model in vivo, and GPR4 antagonist 3b is a very effective tool for investigating the physiologic and pharmacologic roles of GPR4.

Physicochemical Properties

M.Wt 479.672
Formula C31H37N5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-((2-ethyl-5,7-dimethyl-3H-imidazo[4,5-b]pyridin-3-yl)methyl)-8-(piperidin-1-ylmethyl)-10,11-dihydro-5H-dibenzo[b,f]azepine

References

1. Fukuda H, et al. ACS Med Chem Lett. 2016 Feb 24;7(5):493-7.

2. Tobo A, et al. PLoS One. 2015 Jun 12;10(6):e0129334.

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