Home GPCR & G Protein GPR antagonist - cAMP inhibitor - TNF-alpha inhibitor - Interleukins inhibitor - NOS inhibitor - COX inhibitor - PGES inhibitor NE 52-QQ57 For research use only.

NE 52-QQ57

NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).

NE 52-QQ57 Chemical Structure

NE 52-QQ57 Chemical Structure

CAS: 1401728-56-0

Selleck's NE 52-QQ57 has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.72%
99.72

NE 52-QQ57 Related Products

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Biological Activity

Description NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).
Targets
TNF-α [3] IL-1β [3] IL-6 [3] iNOS [3] NO [3] Click to View More Targets

Chemical Information & Solubility

Molecular Weight 416.52 Formula

C24H28N6O
CAS No. 1401728-56-0 SDF --
Smiles CCC1=NN2C(=CC(=NC2=C1CC3=CC=C(C=C3)C4=NN=C(O4)C5CCNCC5)C)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

Ethanol : 45 mg/mL

DMSO : 20 mg/mL ( (48.01 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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