PF 1022A

Modify Date: 2024-01-08 20:32:30

PF 1022A Structure
PF 1022A structure
Common Name PF 1022A
CAS Number 133413-70-4 Molecular Weight 949.17900
Density N/A Boiling Point N/A
Molecular Formula C52H76N4O12 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PF 1022A


PF 1022A is a N-methylated cyclooctadepsipeptides (CODPs) with strong anthelmintic properties; acts as an ionophore.IC50 value:Target: PF 1022A showed strong anthelmintic activities against Ascaridia galli in chickens [1]. PF1022A is a novel anthelmintic that binds to the latrophilin-like transmembrane receptor important for pharyngeal pumping in nematodes. Furthermore, PF1022A binds to GABA receptors, which might contribute to the anthelmintic effect. Like other cyclodepsipeptides, PF1022A acts as an ionophore [2]. In vitro, PF1022A showed low activity on embryonation but significantly inhibited egg hatch (10 and 100 μg/ml), whereas albendazole (10 and 100 μg/ml) revealed statistically significant inhibitions of both embryonation and egg hatch. PF1022A (1-100 μg/ml) completely inhibited larval movement at most examination points [3].

 Names

Name Cyclo[(αR)​-​α-​hydroxybenzenepropan​oyl-​N-​methyl-​L-​leucyl-​(2R)​-​2-​hydroxypropanoyl-​N-​methyl-​L-​leucyl-​(αR)​-​α-​hydroxybenzenepropan​oyl-​N-​methyl-​L-​leucyl-​(2R)​-​2-​hydroxypropanoyl-​N-​methyl-​L-​leucyl]
Synonym More Synonyms

 PF 1022A Biological Activity

Description PF 1022A is a N-methylated cyclooctadepsipeptides (CODPs) with strong anthelmintic properties; acts as an ionophore.IC50 value:Target: PF 1022A showed strong anthelmintic activities against Ascaridia galli in chickens [1]. PF1022A is a novel anthelmintic that binds to the latrophilin-like transmembrane receptor important for pharyngeal pumping in nematodes. Furthermore, PF1022A binds to GABA receptors, which might contribute to the anthelmintic effect. Like other cyclodepsipeptides, PF1022A acts as an ionophore [2]. In vitro, PF1022A showed low activity on embryonation but significantly inhibited egg hatch (10 and 100 μg/ml), whereas albendazole (10 and 100 μg/ml) revealed statistically significant inhibitions of both embryonation and egg hatch. PF1022A (1-100 μg/ml) completely inhibited larval movement at most examination points [3].
Related Catalog
References

[1]. Sasaki T, et al. A new anthelmintic cyclodepsipeptide, PF1022A. J Antibiot (Tokyo). 1992 May;45(5):692-7.

[2]. Dornetshuber R, et al. Effects of the anthelmintic drug PF1022A on mammalian tissue and cells. Biochem Pharmacol. 2009 Apr 15;77(8):1437-44.

[3]. Nwosu U, et al. Efficacy of the cyclooctadepsipeptide PF1022A against Heligmosomoides bakeri in vitro and in vivo. Parasitology. 2011 Aug;138(9):1193-201.

 Chemical & Physical Properties

Molecular Formula C52H76N4O12
Molecular Weight 949.17900
Exact Mass 948.54600
PSA 186.44000
LogP 5.41640
Storage condition 2-8℃

 Synonyms

PF 1022A