PF-1022A

PF-1022A is an anthelmintic depsipeptide isolated from Mycelia Sterilia.

Product information

CAS Number: 133413-70-4

Molecular Weight: 949.18

Formula: C52H76N4O12

Synonym:

PF 1022A

PF1022A

Chemical Name: (3S,6R,9S,12R,15S,18R,21S,24R)-6,18-Dibenzyl-3,9,15,21-tetraisobutyl-4,10,12,16,22,24-hexamethyl-1,7,13,19-tetraoxa-4,10,16,22-tetraazacyclo-tetracosane-2,5,8,11,14,17,20,23-octaone

Smiles: CN1[C@@H](CC(C)C)C(=O)O[C@H](CC2C=CC=CC=2)C(=O)N(C)[C@@H](CC(C)C)C(=O)O[C@H](C)C(=O)N(C)[C@@H](CC(C)C)C(=O)O[C@H](CC2C=CC=CC=2)C(=O)N(C)[C@@H](CC(C)C)C(=O)O[C@H](C)C1=O

InChiKey: YJNUXGPXJFAUQJ-LYWANRAQSA-N

InChi: InChI=1S/C52H76N4O12/c1-31(2)25-39-49(61)65-35(9)45(57)53(11)42(28-34(7)8)52(64)68-44(30-38-23-19-16-20-24-38)48(60)56(14)40(26-32(3)4)50(62)66-36(10)46(58)54(12)41(27-33(5)6)51(63)67-43(47(59)55(39)13)29-37-21-17-15-18-22-37/h15-24,31-36,39-44H,25-30H2,1-14H3/t35-,36-,39+,40+,41+,42+,43-,44-/m1/s1

Technical Data

Appearance: Solid Power.

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

Solubility: Soluble in DMSO

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:

PF 1022A binds to the latrophilin-like transmembrane receptor important for pharyngeal pumping in nematodes. Furthermore, PF 1022A binds to GABA receptors, which might contribute to the anthelmintic effect. In vitro, PF 1022A shows low activity on embryonation but significantly inhibits egg hatch (10 and 100 μg/mL), whereas albendazole (10 and 100 μg/mL) reveales statistically significant inhibitions of both embryonation and egg hatch. PF 1022A (1-100 μg/mL) completely inhibits larval movement at most examination points.

References:

1. von Samson-Himmelstjerna G, Harder A, Schnieder T, Kalbe J, Mencke N. In vivo activities of the new anthelmintic depsipeptide PF 1022A. Parasitol Res. 2000 Mar;86(3):194-9. PubMed PMID: 10726989.
2. Zahner H, Taubert A, Harder A, von Samson-Himmelstjerna G. Filaricidal efficacy of anthelmintically active cyclodepsipeptides. Int J Parasitol. 2001 Nov;31(13):1515-22. PubMed PMID: 11595239.
3. Sivanathan S, Körber F, Scherkenbeck J. Semisynthetic routes to PF1022H--A precursor for new derivatives of the anthelmintic cyclooctadepsipeptide PF1022A. Bioorg Med Chem. 2016 Feb 15;24(4):873-6. doi: 10.1016/j.bmc.2016.01.014. Epub 2016 Jan 8. PubMed PMID: 26810834.

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