Etanercept |
Catalog No.GC34579
One-Click Copy Product Info
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Etanercept is a competitive tumor necrosis factor (TNF) inhibitor that prevents TNF-α and TNF-β from binding to cell surface receptors.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 185243-69-0
Sample solution is provided at 25 µL, 10mM.
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Etanercept is a competitive tumor necrosis factor (TNF) inhibitor that prevents TNF-α and TNF-β from binding to cell surface receptors[1]. Etanercept is effective for rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis[2].
In vitro, Etanercept (1 μg/mL) significantly reduces TNF-α secretion levels in THP-1 cells after 3 hours of treatment following lipopolysaccharide (LPS) stimulation[3].
In vivo, Etanercept (10mg/kg) administered subcutaneously in rats with adjuvant-induced arthritis (AIA) significantly reduces arthritis scores, improves endothelial function and the NOS/BH4/arginase balance, and inhibits the cyclooxygenase-2 (COX-2) pathway[4]. Etanercept (5mg/kg) administered subcutaneously in rats with periodontitis significantly reduces periodontitis inflammation and tissue damage, decreases neutrophil infiltration, and downregulates the expression of apoptotic regulatory factors Bax and Bcl-2[5]. Etanercept (5 mg/kg) administered intraperitoneally in rats with traumatic brain injury (TBI) significantly improves TBI-induced cerebral ischemia, motor and cognitive deficits, inhibits neuronal and glial apoptosis, and reduces levels of inflammatory factors[6].
References:
[1] Alldred A. Etanercept in rheumatoid arthritis[J]. Expert opinion on pharmacotherapy, 2001, 2(7): 1137-1148.
[2] Culy C R, Keating G M. Etanercept: an updated review of its use in rheumatoid arthritis, psoriatic arthritis and juvenile rheumatoid arthritis[J]. Drugs, 2002, 62(17): 2493-2537.
[3] Grattendick K J, Nakashima J M, Feng L, et al. Effects of three anti-TNF-α drugs: etanercept, infliximab and pirfenidone on release of TNF-α in medium and TNF-α associated with the cell in vitro[J]. International immunopharmacology, 2008, 8(5): 679-687.
[4] Totoson P, Maguin-Gaté K, Prigent-Tessier A, et al. Etanercept improves endothelial function via pleiotropic effects in rat adjuvant-induced arthritis[J]. Rheumatology, 2016, 55(7): 1308-1317.
[5] Di Paola R, Mazzon E, Muià C, et al. Effects of etanercept, a tumour necrosis factor‐α antagonist, in an experimental model of periodontitis in rats[J]. British journal of pharmacology, 2007, 150(3): 286-297.
[6] Chio C C, Lin J W, Chang M W, et al. Therapeutic evaluation of etanercept in a model of traumatic brain injury[J]. Journal of neurochemistry, 2010, 115(4): 921-929.
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Cell experiment [1]: |
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Cell lines |
THP-1 cells |
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Preparation method |
Cells were incubated with LPS, Etanercept (1μg/mL), for 3 h, and cell lysates were collected and analyzed for TNF-α. |
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Reaction Conditions |
1μg/mL; 3 h |
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Applications |
Etanercept significantly reduced secreted levels of bioactive TNF-α following stimulation with LPS. |
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Animal experiment [2]: |
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Animal models |
AIA rats |
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Preparation method |
On the day of the first inflammatory symptoms, AIA rats were randomized into two groups. One group received etanercept, at 10 mg/kg (s.c.) every 3 days for 3 weeks (Etanercept, n=30).The other group received saline at 1 ml/kg (s.c.) for 3 weeks (Vehicle, n=30). |
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Dosage form |
10mg/kg; s.c. |
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Applications |
Etanercept significantly reduced arthritis scores, improved endothelial function and NOS/BH4/arginase balance, and inhibited the COX-2 pathway. |
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References: |
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| Cas No. | 185243-69-0 | SDF | |
| Canonical SMILES | [Etanercept] | ||
| Formula | C2224H3475N621O698S36 | M.Wt | 51234.33 |
| Solubility | Soluble in water | Storage | Store at 4°C, Do not freeze |
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 19.5 μL | 97.6 μL | 195.2 μL |
| 5 mM | 3.9 μL | 19.5 μL | 39 μL |
| 10 mM | 2 μL | 9.8 μL | 19.5 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
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Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)