PF-1022A (PF1022A) is a novel and potent N-methylated cyclooctadepsipeptides (CODPs) with excellent anthelmintic properties and acts as an ionophore. PF 1022A showed strong anthelmintic activities against Ascaridia galli in chickens. 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. 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.

Physicochemical Properties

Molecular Formula	C52H76N4O12
Molecular Weight	949.1794
Exact Mass	948.546
Elemental Analysis	C, 65.80; H, 8.07; N, 5.90; O, 20.23
CAS #	133413-70-4
PubChem CID	159590
Appearance	White to off-white solid powder
LogP	5.416
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	12
Rotatable Bond Count	12
Heavy Atom Count	68
Complexity	1580
Defined Atom Stereocenter Count	8
SMILES	O=C(N([C@H](C(O[C@](C(N([C@H](C(O[C@H](CC1=CC=CC=C1)C2=O)=O)CC(C)C)C)=O)([H])C)=O)CC(C)C)C)[C@H](OC([C@@H](N(C([C@H](OC([C@](N2C)([H])CC(C)C)=O)C)=O)C)CC(C)C)=O)CC3=CC=CC=C3
InChi Key	YJNUXGPXJFAUQJ-LYWANRAQSA-N
InChi Code	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
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
Synonyms	PF 1022A; PF-1022A; PF1022A
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	PF 1022A attaches itself to the transmembrane receptor latrophilin-like, which is necessary for pharyngeal pumping in nematodes. PF 1022A additionally binds to GABA receptors, which may enhance the anthelmintic effect[1]. Albendazole (10 and 100 μg/mL) reveals statistically significant inhibitions of both embryonation and egg hatch, while PF 1022A exhibits minimal activity on embryonation but significantly inhibits egg hatch (10 and 100 μg/mL). Larval movement is completely inhibited at most examination points by PF 1022A (1-100 μg/mL)[3].
References	[1]. Effects of the anthelmintic drug PF1022A on mammalian tissue and cells. Biochem Pharmacol. 2009 Apr 15;77(8):1437-44. [2]. A new anthelmintic cyclodepsipeptide, PF1022A. J Antibiot (Tokyo). 1992 May;45(5):692-7. [3]. Efficacy of the cyclooctadepsipeptide PF1022A against Heligmosomoides bakeri in vitro and in vivo. Parasitology. 2011 Aug;138(9):1193-201.
Additional Infomation	PF1022A is a cyclooctadepsipeptide.

Solubility Data

Solubility (In Vitro)

DMSO : ≥ 43 mg/mL (~45.30 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (2.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 10% DMSO+90% Corn Oil: ≥ 2.5 mg/mL (2.63 mM)  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.0535 mL	5.2677 mL	10.5354 mL
	5 mM	0.2107 mL	1.0535 mL	2.1071 mL
	10 mM	0.1054 mL	0.5268 mL	1.0535 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.