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CATPB

Cat. No. M8663

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CATPB Structure

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Quality Control & Documentation
Biological Activity

CATPB is an acetamidophenylbutanoate derivative with inverse agonist and antagonist activity against human, but not mouse or rat, FFA2 (GPR43). CATPB inhibits both constitutive and propionate (C3) -stimulated hFFA2 GTPγS incorporation (IC50 ~35 and 320 nM, respectively; [C3] = EC80, ~125 nM), as well as C3-induced hFFA2 G159E activity (IC50 ~400 nM). CATPB is shown to inhibit C3-induced intracellular ERK phosphorylation in hFFA2-expressing cells (IC50 ~3 μM against 10 mM C3).

Chemical Information
Molecular Weight 399.79
Formula C19H17ClF3NO3
CAS Number 1322598-09-3
Solubility (25°C) DMSO: 10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Simon Lind, et al. Allosteric receptor modulation uncovers an FFA2R antagonist as a positive orthosteric modulator/agonist in disguise

[2] Anders Hjgaard Hansen, et al. Structure-Activity Relationship Explorations and Discovery of a Potent Antagonist for the Free Fatty Acid Receptor 2

[3] Liliana iguez-Gutirrez, et al. Physiological concentrations of short-chain fatty acids induce the formation of neutrophil extracellular traps in vitro

[4] Estela Lorza-Gil, et al. FFA2-, but not FFA3-agonists inhibit GSIS of human pseudoislets: a comparative study with mouse islets and rat INS-1E cells

[5] Zhiwei Ang, et al. FFAR2-FFAR3 receptor heteromerization modulates short-chain fatty acid sensing

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  Catalog
Abmole Inhibitor Catalog




Keywords: CATPB supplier, GPR/FFAR, inhibitors, activators

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