Isoapoptolidin
目录号 : GC43912
Isoapoptolidin is a stable derivative of apoptolidin that demonstrates 10-fold reduced F1FO-ATP synthase inhibitory activity compared to apoptolidin (IC50s = 17 and 0.7 μM, respectively).
Cas No.:476647-30-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >90.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Isoapoptolidin is a stable derivative of apoptolidin that demonstrates 10-fold reduced F1FO-ATP synthase inhibitory activity compared to apoptolidin (IC50s = 17 and 0.7 µM, respectively).
| Cas No. | 476647-30-0 | SDF | |
| Canonical SMILES | O[C@@]([C@]([C@@H](O)C[C@H](OC)[C@@H](O)CC/C=C(C)/C=C/[C@H]1O[C@@]([H])([C@H]2O)O[C@H]([C@@H]([C@H]2O)OC)C)([H])OC(/C(C)=C/C(C)=C/C(C)=C/[C@H]1C)=O)(O[C@@H]3C[C@@H](O[C@@H](C[C@]4(C)O)O[C@H]([C@@H]4O[C@@]([H])(C[C@H]5OC)O[C@@H]([C@H]5O)C)C)COC)[C@H]( | ||
| 分子式 | C58H96O21 | 分子量 | 1129.4 |
| 溶解度 | DMF: Soluble,DMSO: Soluble,Ethanol: Soluble,Methanol: Soluble | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.8854 mL | 4.4271 mL | 8.8543 mL |
| 5 mM | 0.1771 mL | 0.8854 mL | 1.7709 mL |
| 10 mM | 0.0885 mL | 0.4427 mL | 0.8854 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。
Isoapoptolidin: structure and activity of the ring-expanded isomer of apoptolidin
Org Lett 2002 Oct 31;4(22):3819-22.PMID:12599467DOI:10.1021/ol0266222.
[formula: see text] Apoptolidin (1) is a novel oncolytic lead that induces apoptosis in transformed cell lines with exceptional selectivity. We report the isolation and characterization of a ring-expanded macrolide isomer of apoptolidin: Isoapoptolidin (2). The solution conformation of Isoapoptolidin is described. The rate of isomerization was measured under biologically relevant conditions and found to approach equilibrium within the time frame of most cell-based assays. Isoapoptolidin's ability to inhibit mitochondrial F0F1-ATPase is over 10-fold less than that of apoptolidin.
Toward a stable apoptolidin derivative: identification of Isoapoptolidin and selective deglycosylation of apoptolidin
Org Lett 2002 Oct 31;4(22):3823-5.PMID:12599468DOI:10.1021/ol026829v.
[formula: see text] Isoapoptolidin was isolated from crude fermentation extracts of the apoptolidin-producing microorganism Nocardiopsis sp. Apoptolidin isomerizes to Isoapoptolidin upon treatment with methanolic triethylamine to establish a 1.4:1 equilibrium mixture of Isoapoptolidin and apoptolidin. Semisynthesis of a peracetylated and deglycosylated derivative of apoptolidin is also described.
Isolation, structure determination, and anti-cancer activity of apoptolidin D
Org Lett 2007 Feb 15;9(4):691-4.PMID:17286376DOI:10.1021/ol0630245.
The isolation, characterization, and preliminary biological activity of apoptolidin D, a new apoptolidin that exhibits anti-proliferative activity against H292 human lung carcinoma cells at nanomolar concentrations, are reported. Its equilibration with Isoapoptolidin D and characterization of the latter are also described. [structure: see text].