| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
Purity: ≥98%
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.
| Targets |
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]. |
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| 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]. PF-1022A was tested for antimicrobial activity and showed no activity against Gram-positive bacteria, Gram-negative bacteria, yeasts, and other fungi at a dose of 100 µg/ml. [2] |
| ln Vivo |
PF-1022A exhibited potent anthelmintic activity against the nematode Ascaris galli (chicken roundworm) in an in vivo chicken model.
Oral administration of PF-1022A at a dose of 2 mg/kg resulted in 91.7% to 100% efficacy in expelling worms from infected chickens. The anthelmintic activity was dose-dependent, with lower efficacy observed at 0.5 mg/kg (9.7% to 24.1%) and 1.0 mg/kg (33.3% to 76.0%). No toxic effects were observed in the host chickens at the tested doses. [2] |
| Animal Protocol |
Anthelmintic efficacy study in chickens: One-week-old chickens were orally infected with 200 eggs of Ascaris galli.
Thirty-five days post-infection, the infected chickens were orally administered a single dose of PF-1022A. The doses tested were 0.5, 1.0, and 2.0 mg/kg. The formulation/vehicle for oral administration is not specified. For the next two weeks following drug administration, feces were collected daily, and the number of worms excreted was counted. Two weeks after drug administration, all chickens were sacrificed, and the gastrointestinal tracts were examined to count the number of remaining worms. The experiment was conducted in triplicate (n=3 chickens) for each dose group. Efficacy rate was calculated as: (Number of worms excreted / Total number of worms [excreted + remaining]) × 100%. [2] Acute toxicity study in mice: PF-1022A was administered to mice intraperitoneally (i.p.) at a dose of 1 g/kg and orally (p.o.) at a dose of 2 g/kg. No acute toxicity was observed at these doses. The formulation/vehicle is not specified. [2] |
| Toxicity/Toxicokinetics |
In acute toxicity studies in mice, no toxicity was observed after intraperitoneal injection of 1 g/kg PF-1022A or oral administration of 2 g/kg PF-1022A. In anthelmintic efficacy studies in chickens, no toxic effects were observed in host animals at therapeutic doses (0.5, 1.0, and 2.0 mg/kg). Other toxicity endpoints (e.g., organ toxicity, plasma protein binding) were not described. [2]
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| References | |
| Additional Infomation |
PF1022A is a cyclooctapeptide. PF-1022A is a novel cyclic peptide antibiotic isolated from the cultured mycelium of the fungus Mycelia Sterilia PF1022 (FERM BP-2671). Its structure has been determined to be cyclo(D-lactyl-LN-methylleucyl-D-3-phenyllactyl-LN-methylleucyl-D-lactyl-LN-methylleucyl-D-3-phenyllactyl-LN-methylleucyl). It consists of two D-lactic acid (Lac) units, two D-3-phenyllactic acid (Phi) units, and four LN-methylleucine (MeLeu) units arranged in an alternating ring. It is a neutral substance, soluble in organic solvents such as methanol, acetone, and chloroform, but insoluble in water. The structure of this compound is similar to that of the known insecticidal cyclic peptide compound, bassianolide. It is a promising anthelmintic that can be used to treat parasitic nematode infections. [2]
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| Molecular Formula |
C52H76N4O12
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|---|---|
| Molecular Weight |
949.1794
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| Exact Mass |
948.546
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| Elemental Analysis |
C, 65.80; H, 8.07; N, 5.90; O, 20.23
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| CAS # |
133413-70-4
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| PubChem CID |
159590
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| Appearance |
White to off-white solid powder
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| LogP |
5.416
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
68
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| Complexity |
1580
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| Defined Atom Stereocenter Count |
8
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| 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
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| InChi Key |
YJNUXGPXJFAUQJ-LYWANRAQSA-N
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| 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
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| 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
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| Synonyms |
PF 1022A; PF-1022A; PF1022A
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ≥ 43 mg/mL (~45.30 mM)
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| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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