Vinflunine Tartrate

目录号: GC13815纯度: >98%同义词: 长春氟宁酒石酸盐

Etanercept is an inhibitor of the inflammatory factor TNF-α and is mainly used for the clinical treatment of rheumatoid arthritis .


Vinflunine Tartrate
Cas No.: 1201898-17-0
规格价格库存数量操作
5mg¥924.00现货
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10mg¥1,554.00现货
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50mg¥4,788.00现货
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200mg¥13,167.00现货
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产品描述 Description

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.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Human retinal microvascular endothelial cells (HRECs)

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).

Reaction Conditions

20 or 50 µg/mL;7 h

Applications

Etanercept reduces endothelial tube formation.

Animal experiment [2]:

Animal models

30 day-old Wistar albino rats(50-70 g)

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

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.

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.
[2].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.

产品文档 Product Documents

化学性质Chemical Properties

CAS 号
1201898-17-0
同义词
长春氟宁酒石酸盐
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 g/mol
溶解性
Soluble in DMSO > 10 mM
保存条件
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°C,然后在超声波浴中震荡一段时间。
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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

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