DC260126

DC260126 is a potent antagonist of GPR40 (FFAR1). DC260126 dose-dependently inhibits GPR40-mediated Ca2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50: 6.28, 5.96, 7.07, 4.58 μM, respectively). DC260126 could protect MIN6 β cells from palmitate-induced ER stress and apoptosis.

Product information

CAS Number: 346692-04-4

Molecular Weight: 307.38

Formula: C16H18FNO2S

Chemical Name: N-(4-butylphenyl)-4-fluorobenzene-1-sulfonamide

Smiles: CCCCC1C=CC(=CC=1)NS(=O)(=O)C1C=CC(F)=CC=1

InChiKey: CNGHPXKWPGIDSK-UHFFFAOYSA-N

InChi: InChI=1S/C16H18FNO2S/c1-2-3-4-13-5-9-15(10-6-13)18-21(19,20)16-11-7-14(17)8-12-16/h5-12,18H,2-4H2,1H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 100 mg/mL (325.33 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

DC260126 reduces GTP-loading and ERK1/2 phosphorylation stimulated by linoleic acid in GPR40-CHO cells, suppresses palmitic acid potentiated glucose-stimulated insulin secretion, and negatively regulates GPR40 mRNA expression induced by oleic acid in Min6 cells.

References:

1. Hu H, et al. A novel class of antagonists for the FFAs receptor GPR40. Biochem Biophys Res Commun. 2009;390(3):557-563.
2. Wu J, et al. Inhibition of GPR40 protects MIN6 β cells from palmitate-induced ER stress and apoptosis [published correction appears in J Cell Biochem. 2013 May;114(5):1216]. J Cell Biochem. 2012;113(4):1152-1158.

Products are for research use only. Not for human use.