Vinflunine Tartrate
(Synonyms: 长春氟宁酒石酸盐) 目录号 : GC13815
Etanercept is an inhibitor of the inflammatory factor TNF-α and is mainly used for the clinical treatment of rheumatoid arthritis .
Cas No.:1201898-17-0
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
| Cell experiment [1]: | |
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Cell lines |
Human retinal microvascular endothelial cells (HRECs) |
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Preparation Method |
Melted Matrigel Matrix was added to a 96-well plate at 100 µL per well and allowed to stand in an incubator (37¡橠for 30 min. The HRECs were evenly spread on the Matrigel Matrix on ice. Different concentrations of etanercept or PBS were added to the cells 60 min before the addition of the human recombinant TNF-α (rhTNF-α). The concentration of rhTNF-α was 1 ng/mL and that of etanercept was 20 or 50 µg/mL. The plate was placed at 37¡栦or 7 h, cell tube formation images were captured with an inverted microscope (100x). |
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Reaction Conditions |
20 or 50 µg/mL;7 h |
|
Applications |
Etanercept reduces endothelial tube formation. |
| Animal experiment [2]: | |
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Animal models |
30 day-old Wistar albino rats(50-70 g) |
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Preparation Method |
Rats were separated into the three groups: contro, CD, and CD + ETA (exposed to CD and treated with subcutaneous injections of etanercept (0.8 mg/kg/week) for 12 weeks). The control group was fed with a standard pellet diet. The CD and CD + ETA groups were fed with CD, which is a high-fat diet |
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Dosage form |
0.8 mg/kg/week; 12 weeks; s.c. |
|
Applications |
12-week chronic etanercept treatment significantly restored endothelium-dependent vasorelaxation and resulted in decreased serum levels of TNF-α and increased eNOS expression in rats exposed to CD. |
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References: [1]. Yao Y, Cai Y,et,al. Etanercept as a TNF-alpha inhibitor depresses experimental retinal neovascularization. Graefes Arch Clin Exp Ophthalmol. 2021 Mar;259(3):661-671. doi: 10.1007/s00417-020-04956-6. Epub 2020 Oct 12. PMID: 33043386. |
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Etanercept is an inhibitor of the inflammatory factor TNF-α and is mainly used for the clinical treatment of rheumatoid arthritis (RA), ankylosing spondylitis, and uveitis [1-3]. Etanercept can competitively inhibit the binding of two subtypes of TNF (TNF-α and TNF-β) to their cell surface receptor (TNFR) and further prevent TNF-α and TNF-β from exerting their biological effects [4].
In vitro, etanercept(20 or 50 µg/mL;7 h) reduced endothelial cell tube formation by inhibiting activation of the NF-κB signaling pathway[7]. The protective effect of etanercept(24h)lies in the restoration of autophagy against TNF-induced endothelial damage in EA.hy926 endothelial cells [5].
Etanercept treatment(0.8 mg/kg/week; 12 weeks;i.p.) significantly restored endothelium-dependent vasorelaxation and resulted in decreased serum levels of TNF-α and increased eNOS expression in rats exposed to CD[6].
References:
[1]. Padilla-Mart EM, Romero SC, et,al. (2019) Drug levels and antibodies against TNF-blockers in spondyloarthritis and rheumatoid arthritis are associated with the activity but they do not predict it. Curr Rheumatol Rev 15:329-335
[2]. D'Adamio S, Silvaggio D, et,al. Pharmacotherapeutic management of psoriasis in adolescents and children. Expert Opin Pharmacother. 2019 Oct;20(14):1777-1785. doi: 10.1080/14656566.2019.1636032. Epub 2019 Jul 4. PMID: 31271541.
[3]. Bartalena L. Commentary: rituximab, adalimumab, etanercept, tocilizumab--are biologics the future for Graves' orbitopathy? Ophthalmic Plast Reconstr Surg. 2014 Sep-Oct;30(5):420-3. doi: 10.1097/IOP.0000000000000221. PMID: 25025391.
[4]. Lim H, Lee SH, et,al. Structural Biology of the TNFα Antagonists Used in the Treatment of Rheumatoid Arthritis. Int J Mol Sci. 2018 Mar 7;19(3):768. doi: 10.3390/ijms19030768. PMID: 29518978; PMCID: PMC5877629.
[5]. Barbati C, Colasanti T, et,al. Up-regulation of autophagy by etanercept treatment results in TNF-induced apoptosis reduction in EA.hy926 endothelial cell line. Clin Exp Rheumatol. 2021 May-Jun;39(3):606-611. doi: 10.55563/clinexprheumatol/uiqdtq. Epub 2020 Sep 3. PMID: 32896251.
[6]. R?zvan-Valentin S, GÜler SA, et,al. Etanercept Prevents Endothelial Dysfunction in Cafeteria Diet-Fed Rats. Int J Environ Res Public Health. 2022 Feb 14;19(4):2138. doi: 10.3390/ijerph19042138. PMID: 35206342; PMCID: PMC8872388.
[7]. Yao Y, Cai Y, et,al. Etanercept as a TNF-alpha inhibitor depresses experimental retinal neovascularization. Graefes Arch Clin Exp Ophthalmol. 2021 Mar;259(3):661-671. doi: 10.1007/s00417-020-04956-6. Epub 2020 Oct 12. PMID: 33043386.
| Cas No. | 1201898-17-0 | SDF | |
| 别名 | 长春氟宁酒石酸盐 | ||
| Canonical SMILES | [H][C@]12[C@]3(CC)[C@@H](OC(C)=O)[C@](O)(C(OC)=O)[C@]4([H])N(C)C5=CC(OC)=C([C@](C[C@H]6C[C@@H](C(F)(F)C)CN7C6)(C(OC)=O)C8=C(C7)C(C=CC=C9)=C9N8)C=C5[C@@]41CCN2CC=C3.O=C(O)[C@H](O)[C@@H](O)C(O)=O | ||
| 分子式 | C45H54F2N4O8.xC4H6O6 | 分子量 | 967.02 |
| 溶解度 | Soluble in DMSO > 10 mM | 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 | 1.0341 mL | 5.1705 mL | 10.341 mL |
| 5 mM | 0.2068 mL | 1.0341 mL | 2.0682 mL |
| 10 mM | 0.1034 mL | 0.5171 mL | 1.0341 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。
[Characterization of vinflunine tartrate liposomes in vitro and in vivo]
Vinflunine tartrate-loaded liposomes (VT-L) with two drug-to-lipid ratios were prepared by pH gradient method. Vesicle size and zeta potential were determined by the Zetasizer Nano ZS. Entrapment efficiency was evaluated by cation exchange resin centrifugalization method. The toxicity and tumor inhibition to nude mouse administrated by VT-L with different drug-to-lipid ratios were investigated and compared with the vinflunine tartrate injection (VT-I). The results showed that the mean particle size, zeta potential and entrapment efficiency of the VT-L with drug-to-lipid ratios of 1 : 5 and 1 : 10 were 124.6 nm and 128.3 nm, -25.3 mV and -22.8 mV, 94.46% and 97.31%, respectively. The VT-L with two different drug-to-lipid ratios has significantly higher anti-tumor effect to nude mouse transplanted human non-small cell lung carcinoma A549 and lower toxicity than VT-I. While there were no significant differences in anti-tumor effect and toxicity between VT-L with two different drug-to-lipid ratios.