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R-7050

Catalog No. T4637   CAS 303997-35-5
Synonyms: TNF-α Antagonist III

R-7050 (TNF-α Antagonist III), a tumor necrosis factor receptor (TNFR) antagonist, exhibits heightened selectivity for TNFα.

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R-7050 Chemical Structure
R-7050, CAS 303997-35-5
Pack Size Availability Price/USD Quantity
2 mg In stock $ 38.00
5 mg In stock $ 61.00
10 mg In stock $ 97.00
25 mg In stock $ 217.00
50 mg In stock $ 297.00
100 mg In stock $ 488.00
500 mg In stock $ 1,060.00
1 mL * 10 mM (in DMSO) In stock $ 68.00
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Purity: 99.14%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description R-7050 (TNF-α Antagonist III), a tumor necrosis factor receptor (TNFR) antagonist, exhibits heightened selectivity for TNFα.
In vitro R-7050 is a cell-permeable triazoloquinoxaline compound that selectively inhibits TNF-α induced cellular signaling. Unlike biologic TNF inhibitors (e.g. Infliximab, Etanercept, Adalimumab) that directly bind TNF-α and function as decoy receptors, R-7050 does not affect binding of TNF-α to TNFR. In contrast, R-7050 selectively inhibits the association of TNFR with intracellular adaptor molecules (e.g. TRADD, RIP), limits receptor internalization, and prevents subsequent cellular responses after TNF-α binding[2].
In vivo Administered at doses of 6 mg/kg, R-7050 significantly attenuates Evans blue extravasation in brain tissue to 28.7±5.9 μg and 30.3±1.9 μg when given 0.5 hours or 2 hours after induced intracerebral hemorrhage (ICH), respectively, presenting statistical significance (p<0.05 and p<0.01 vs ICH, respectively) and comparability to sham-operated controls. Concurrently, brain water content, indicative of brain edema, increases markedly from 75.6±0.3% in sham to 81.5±0.5% post-ICH (p<0.05 vs. sham). Doses of R-7050 (6, 12, or 18 mg/kg) effectively reduce the brain water content to 78.5±0.3%, 78.3±0.3%, and 79.3±0.5%, respectively, each significantly against ICH (p<0.05) and with no significant difference among the dosages. However, a notable decrease in general activity/locomotion is observed with the highest dose (18 mg/kg). R-7050, at a 6 mg/kg dosage, also significantly mitigates the increase in brain water content post-ICH to levels akin to those in sham-operated mice (p<0.05 vs ICH and not significantly different from sham), demonstrating its potential in reducing both brain edema and permeability post-ICH when administered timely.
Synonyms TNF-α Antagonist III
Molecular Weight 380.77
Formula C16H8ClF3N4S
CAS No. 303997-35-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (26.26 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Gururaja TL, et al. A class of small molecules that inhibit TNFalpha-induced survival and death pathways viaprevention of interactions between TNFalphaRI, TRADD, and RIP1. Chem Biol. 2007 Oct;14(10):1105-18. 2. King MD, et al. TNF-alpha receptor antagonist, R-7050, improves neurological outcomes following intracerebralhemorrhage in mice. Neurosci Lett. 2013 May 10;542:92-6.

TargetMolCitations

1. Yi Y, Gao K, Lin P, et al. Staphylococcus aureus-Induced Necroptosis Promotes Mitochondrial Damage in Goat Endometrial Epithelial Cells. Animals. 2022, 12(17): 2218.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Active Compound Library Angiogenesis related Compound Library Apoptosis Compound Library Anti-Fibrosis Compound Library Pyroptosis Compound Library Anti-Cardiovascular Disease Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Bioactive Compound Library

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Keywords

R-7050 303997-35-5 Apoptosis TNF Inhibitor TNF-a Antagonist III inhibit TNFR Tumor Necrosis Factor Receptor TNF Receptor TNF-α Antagonist III R7050 R 7050 TNF-alpha Antagonist III inhibitor

 

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