PF 1022A
目录号 : GC14630
A cyclodepsipeptide with anthelmintic activity
Cas No.:133413-70-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
PF1022A is a novel anthelmintic cyclodepsipeptide. It was isolated from cultured mycelia of PF1022 Mycelia Sterilia, and exhibited strong anthelmintic activities against Ascaridia galli in chickens. [2] PF1022A seems to be a safe alternative to other anthelmintic drugs [1].
PF1022 is consisted of four alternating residues of N-methyl-L-leucine and four residues of D-phenyl-lactate or D-lactate [3]. PF1022A binds to the latrophilin-like transmembrane receptor and is important for pharyngeal pumping in nematodes. Furthermore, PF1022A binds to GABA receptors, which might contribute to the anthelmintic effect. PF1022A acts as an ionophore. In necrotic cells, PF1022A did not induce cell death indicated by lack of cellular lactate dehydrogenase release. PF1022A-induced cytotoxicity is impacted on the cell cycle and apoptosis regulating proteins p53, bax and p21, but not Bcl-2.
The efficacy of PF 1022A was investigated against the following parasite species: Strongyloides ratti and Nippostrongylus brasiliensis in rats, Ancylostoma caninum in dogs, Trichostrongylus colubriformis and Haemonchus contortus in sheep, small strongyles (cyathostomes) in horses, and Dictyocaulus viviparus in cattle. Oral, subcutaneous or intravenous application at doses varied from 1 to 10 mg/kg body weight was compared in livestock animals. High degrees of efficacy were found in all the above-cited examinations, and no clinical signs of impatience were observed. [4]
References:
[1].Dornetshuber R, Kamyar MR, Rawnduzi P et al. Effects of the anthelmintic drug PF1022A on mammalian tissue and cells. Biochem Pharmacol. 2009 Apr 15;77(8):1437-44.
[2].Sasaki T, Takagi M, Yaguchi T et al. A new anthelmintic cyclodepsipeptide, PF1022A. J Antibiot (Tokyo). 1992 May;45(5):692-7.
[3].Yanai K, Sumida N, Okakura K et al. Para-position derivatives of fungal anthelmintic cyclodepsipeptides engineered with Streptomyces venezuelae antibiotic biosynthetic genes. Nat Biotechnol. 2004 Jul;22(7):848-55. Epub 2004 Jun 6.
[4].Von Samson-Himmelstjerna G, Harder A, Schnieder T. In vivo activities of the new anthelmintic depsipeptide PF 1022A. Parasitol Res. 2000 Mar;86(3):194-9.
| Cas No. | 133413-70-4 | SDF | |
| 化学名 | (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-tetraazacyclotetracosan-2,5,8,11,14,17,20,23-octaone | ||
| Canonical SMILES | O=C([C@@H](CC1=CC=CC=C1)OC([C@H](CC(C)C)N(C)C2=O)=O)N(C)[C@H](C(O[C@H](C)C(N(C)[C@H](C(O[C@H](CC3=CC=CC=C3)C(N(C)[C@H](C(O[C@@H]2C)=O)CC(C)C)=O)=O)CC(C)C)=O)=O)CC(C)C | ||
| 分子式 | C52H76N4O12 | 分子量 | 949.18 |
| 溶解度 | ≥ 31.75mg/mL in DMSO | 储存条件 | Desiccate at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。