Lanopepden (GSK 1322322)
(Synonyms: GSK 1322322) 目录号 : GC32311
Lanopepden (GSK 1322322) (GSK 1322322) 是一种肽去甲酰基酶抑制剂，对金黄色葡萄球菌菌株具有活性，对 ATCC 29213 和 ATCC 25923 菌株的 MIC 分别为 1 和 1 mg/L。
Cas No.:1152107-25-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Lanopepden (GSK 1322322) is a peptide deformylase inhibitor active against Staphylococcus aureus strains with MICs of 1 and 1 mg/L for ATCC 29213 and ATCC 25923 strain, respectively[1].
[1]. Peyrusson F, et al. Cellular pharmacokinetics and intracellular activity of the novel peptide deformylase inhibitor GSK1322322 against Staphylococcus aureus laboratory and clinical strains with various resistance phenotypes: studies with human THP-1 monocytes and J774 murine macrophages. Antimicrob Agents Chemother. 2015 Sep;59(9):5747-60.
| Cas No. | 1152107-25-9 | SDF | |
| 别名 | GSK 1322322 | ||
| Canonical SMILES | FC1=C(N2CCN(CCOC3)[C@@]3([H])C2)N=C(C)N=C1NNC([C@H](CC4CCCC4)CN(C=O)O)=O | ||
| 分子式 | C22H34FN7O4 | 分子量 | 479.55 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store 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 | 2.0853 mL | 10.4264 mL | 20.8529 mL |
| 5 mM | 0.4171 mL | 2.0853 mL | 4.1706 mL |
| 10 mM | 0.2085 mL | 1.0426 mL | 2.0853 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。
Peptide deformylase: a new target in antibacterial, antimalarial and anticancer drug discovery
Curr Med Chem 2015;22(2):214-36.PMID:25174923DOI:10.2174/0929867321666140826115734
Peptide deformylase (PDF) is a class of metalloenzyme responsible for catalyzing the removal of the N-formyl group from N-terminal methionine following translation. PDF inhibitors are moving into new phase of drug development. Initially, PDF was considered as an important target in antibacterial drug discovery; however genome database searches have revealed PDF-like sequences in parasites (P. falciparum) and human, widening the utility of this target in antimalarial and anticancer drug discovery along with antibacterial. Using structural and mechanistic information together with high throughput screening, several types of chemical classes of PDF inhibitors with improved efficacy and specificity have been identified. Various drugs like, GSK-1322322 (Phase II), BB-83698 (Phase I), and LBM-415 (Phase I) have entered into clinical developments. Developments in the field have prompted us to review the current aspects of PDFs, especially their structures, different classes of PDF inhibitors, and molecular modeling studies. In nut shell, this review enlightens PDF as a versatile target along with its inhibitors and future perspectives of different PDF inhibitors.