R-7050 (Synonyms: TNF-α Antagonist III) |
Catalog No.GC11659
One-Click Copy Product Info
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R-7050 is a cell-permeable tumor necrosis factor receptor (TNFR) antagonist with higher selectivity for TNF-α.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 303997-35-5
Sample solution is provided at 25 µL, 10mM.
R-7050 is a cell-permeable tumor necrosis factor receptor (TNFR) antagonist with higher selectivity for TNF-α[1]. TNF-α is a key mediator of immune and inflammatory responses, mediating host defense at physiological concentrations, while its overproduction can induce tissue damage and autoimmune pathology[2,3]. R-7050 has been extensively utilized in studies related to autoimmune diseases, neuroinflammation (such as intracerebral hemorrhage models), and the tumor microenvironment[4,5].
In vitro, mouse brain endothelial bEnd.3 cells were pretreated with R-7050 (5μM) for 30min and then incubated with TNF-α (50ng/mL) for an additional 24h, effectively reversing the TNF-α-induced decrease in transendothelial electrical resistance (TEER)[6].
In vivo, R-7050 (5mg/kg) administered via intraperitoneal injection 30min prior to ischemia in a rat model of permanent cerebral ischemia reduced cerebral infarction volume at 24h post-ischemia[6]. R-7050 (6mg/kg) administered as a single intraperitoneal injection at 0.5h or 2h after intracerebral hemorrhage in CD-1 mice effectively attenuated blood-brain barrier disruption at 24h post-hemorrhage[7].
References:
[1] Mizuno S, Osaki E, Ohnishi H. TNF type-I receptor inhibitor, R-7050 attenuates acute kidney injury in a mouse model of crush syndrome. Pharmacol Pharm. 2018;9(12):547-8.
[2] Idrus H H, Budu H M. Biological effects of tumor necrosis factor alpha (TNF-α) in systemic inflammation[J]. Int. J. Med. Sci. Dent. Res, 2020, 3(3): 7-15.
[3] Jang D, Lee A H, Shin H Y, et al. The role of tumor necrosis factor alpha (TNF-α) in autoimmune disease and current TNF-α inhibitors in therapeutics[J]. International journal of molecular sciences, 2021, 22(5): 2719.
[4] Ma Y, Cheng Q, Wang E, et al. Inhibiting tumor necrosis factor‑α signaling attenuates postoperative cognitive dysfunction in aged rats[J]. Molecular Medicine Reports, 2015, 12(2): 3095-3100.
[5] Wen Y, Lu X, Ren J, et al. KLF4 in macrophages attenuates TNFα-mediated kidney injury and fibrosis[J]. Journal of the American Society of Nephrology: JASN, 2019, 30(10): 1925.
[6] Lin S Y, Wang Y Y, Chang C Y, et al. TNF-α receptor inhibitor alleviates metabolic and inflammatory changes in a rat model of ischemic stroke[J]. Antioxidants, 2021, 10(6): 851.
[7] King M D, Alleyne Jr C H, Dhandapani K M. TNF-alpha receptor antagonist, R-7050, improves neurological outcomes following intracerebral hemorrhage in mice[J]. Neuroscience letters, 2013, 542: 92-96.
| Cell experiment [1]: | |
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Cell lines |
bEnd.3 cells |
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Preparation Method |
bEnd.3 cells were pretreated with R-7050 (5μM) for 30min before being incubated with TNF-α (50ng/mL) for an additional 24h. Endothelial barrier integrity was assessed by measuring TEER using a Millicell ERS ohmmeter. |
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Reaction Conditions |
5μM; 30min and additional 24h |
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Applications |
Pretreatment with R-7050 can effectively reverse the decrease of TEER induced by TNF-α. |
| Animal experiment [1]: | |
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Animal models |
Rat model of permanent cerebral ischemia |
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Preparation Method |
Rats were pretreated with a single intraperitoneal injection of R-7050 (5mg/kg) 30min before permanent cerebral ischemia. Brain infarction volume was assessed by triphenyltetrazolium chloride (TTC) staining at 24h after ischemia. |
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Dosage form |
5mg/kg; i.p. |
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Applications |
Pretreatment with R-7050 reduced the cerebral infarction volume of rats with permanent cerebral ischemia after 24h of ischemia. |
References: [1] Lin S Y, Wang Y Y, Chang C Y, et al. TNF-α receptor inhibitor alleviates metabolic and inflammatory changes in a rat model of ischemic stroke[J]. Antioxidants, 2021, 10(6): 851. | |
| Cas No. | 303997-35-5 | SDF | |
| Synonyms | TNF-α Antagonist III | ||
| Chemical Name | 8-chloro-4-(phenylthio)-1-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]quinoxaline | ||
| Canonical SMILES | ClC1=CC(N2C3=NN=C2C(F)(F)F)=C(C=C1)N=C3SC4=CC=CC=C4 | ||
| Formula | C16H8ClF3N4S | M.Wt | 380.8 |
| Solubility | DMSO (warmed with 50ºC water bath) 9 mg/mL (23.64 mM) ; DMF: 10 mg/ml | Storage | Store at -20°C |
| 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 | 2.6261 mL | 13.1303 mL | 26.2605 mL |
| 5 mM | 525.2 μL | 2.6261 mL | 5.2521 mL |
| 10 mM | 262.6 μL | 1.313 mL | 2.6261 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)