| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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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.
| 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]. |
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| References | |
| Additional Infomation |
PF1022A is a cyclooctadepsipeptide.
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| Molecular Formula |
C52H76N4O12
|
|---|---|
| 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
|
| 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
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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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