Drug intelligence / Profile preview

FPL 67156

Development stage
Preclinical
Lead developer
Sanofi
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
In Vitro, Laboratory Use; No Established Clinical Route
01

Overview

FPL 67156 is a small molecule ecto-ATPase inhibitor, specifically an analogue of ATP, with the chemical structure 6-N,N-diethyl-beta,gamma-dibromomethylene-D-ATP. It inhibits ecto-ATPases (including NTPDases such as CD39), thereby preventing the breakdown of extracellular ATP and other nucleotides. This potentiates the effects of nucleotides like ATP and UTP at various purinoceptors, influencing physiological responses like chloride secretion and vascular contractility. FPL 67156 has weak antagonistic effects at P2X and P2T purinoceptors, and weak agonistic effects at P2U purinoceptors. It is primarily used as a research tool to study nucleotide signaling and purinoceptor classification.[1][3][4][10]

Other names
6-N,N-diethyl-beta,gamma-dibromomethylene-D-ATP6-N,N-diethyl-D-beta,gamma-dibromomethyleneATPARL 67156 trisodium saltARL67156 trisodium saltARL-67156 trisodium salt
02

Targets

NTPDase3 (Ectonucleoside triphosphate diphosphohydrolase 3)ENTPD2 (Ectonucleoside triphosphate diphosphohydrolase 2)ENPP1NT5E (Cluster of Differentiation 73)ENPP3 (Ectonucleotide pyrophosphatase/phosphodiesterase 3)ENTPD1 (Ectonucleoside triphosphate diphosphohydrolase 1)NTPDase8 (Ectonucleoside triphosphate diphosphohydrolase 8)

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