Heparastatin
(Synonyms: SF4) 目录号 : GC31531
An inhibitor of heparanase
Cas No.:153758-25-9
Sample solution is provided at 25 µL, 10mM.
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Heparastatin is an inhibitor of heparanase, an enzyme that cleaves heparan sulfate into glucuronic acid (GlcUA) and N-acetylglucosamine (GlcNAc).1 It inhibits heparanase in A375-M human melanoma cells expressing the recombinant human enzyme (IC50 = 10.55 ?M). Heparastatin also inhibits bovine liver β-glucuronidase and almond β-glucosidase (IC50s = 0.31 and 11 ?M, respectively). It reduces air pouch neutrophil and monocyte infiltration and levels of chemokine (C-C motif) ligand 2 (CCL2) in a mouse model of dorsal air pouch inflammation induced by carrageenan.2 Heparastatin (100 mg/kg once per day) inhibits metastasis by 57.1% in a murine Lewis lung carcinoma model.3
1.Nishimura, Y., Shitara, E., Adachi, H., et al.Flexible synthesis and biological activity of uronic acid-type gem-diamine 1-N-iminosugars: A new family of glycosidase inhibitorsJ. Org. Chem.65(1)2-11(2000) 2.Sue, M., Higashi, N., Shida, H., et al.An iminosugar-based heparanase inhibitor heparastatin (SF4) suppresses infiltration of neutrophils and monocytes into inflamed dorsal air pouchesInt. Immunopharmacol.3515-21(2016) 3.Nishimura, Y., Satoh, T., Kondo, S., et al.Effect on spontaneous metastasis of mouse Lewis lung carcinoma by a trifluoroacetamide analogue of siastatin BJ. Antibiot. (Tokyo)47(7)840-842(1994)
Cell experiment: | Influence of a heparanase inhibitor on TGF-β3-induced EMT of NMuMG cells. NMuMG cells are cultured with 1 ng/mL TGF-β3 together with 10 or 100 μM Heparastatin (SF4) for 48 h[2]. |
References: [1]. Sue M, et al. An iminosugar-based heparanase inhibitor heparastatin (SF4) suppresses infiltration of neutrophils and monocytes into inflamed dorsal air pouches. Int Immunopharmacol. 2016 Jun;35:15-21. | |
| Cas No. | 153758-25-9 | SDF | |
| 别名 | SF4 | ||
| Canonical SMILES | O=C([C@H]1CN[C@H](NC(C(F)(F)F)=O)[C@@H](O)[C@H]1O)O | ||
| 分子式 | C8H11F3N2O5 | 分子量 | 272.18 |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.674 mL | 18.3702 mL | 36.7404 mL |
| 5 mM | 0.7348 mL | 3.674 mL | 7.3481 mL |
| 10 mM | 0.3674 mL | 1.837 mL | 3.674 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet