Vinflunine Tartrate |
| Catalog No.GC13815 |
Etanercept is an inhibitor of the inflammatory factor TNF-α and is mainly used for the clinical treatment of rheumatoid arthritis .
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1201898-17-0
Sample solution is provided at 25 µL, 10mM.
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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]. Răzvan-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.
| 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℃) 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℃ for 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. |
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| Cas No. | 1201898-17-0 | SDF | |
| 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 | ||
| Formula | C45H54F2N4O8.xC4H6O6 | M.Wt | 967.02 |
| Solubility | Soluble in DMSO > 10 mM | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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