TNF-α Antagonist III
R-7050(TNF-α Antagonist III)
CAS: 303997-35-5
Molecular Formula: C16H8ClF3N4S
TNF-α Antagonist III - Names and Identifiers
TNF-α Antagonist III - Physico-chemical Properties
| Molecular Formula | C16H8ClF3N4S |
| Molar Mass | 380.77 |
| Density | 1.59±0.1 g/cm3(Predicted) |
| Solubility | DMSO : 25 mg/mL (65.66 mM; Need ultrasonic) |
| pKa | -3.70±0.30(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| In vitro study | R-7050 (TNF-α Antagonist III) is a potent and fully reversible hit with greater selectivity toward TNFα. In TNFα-induced intercellular adhesion molecule 1 (ICAM-1) expression, R-7050 inhibition potency (EC 50 =0.63 μM) is 2- to 3-fold greater than EC 50 for IL-1β-induced ICAM-1 expression (EC 50 =1.45 2 μM). R-7050 inhibits phosphorylation of both the JNK pathway (MKK4, JNKs, and ATF2) and p38 pathway (MKK3/6, p38, and MAPKAP2). 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. |
| In vivo study | R-7050 (TNF-α Antagonist III) (6 mg/kg) reduces Evans blue extravasation to 28.7±5.9 μg and 30.3±1.9 μg Evans blue/g brain tissue when administered at 0.5 h or 2 h post-ICH, respectively (p<0.05 and p<0.01 vs ICH, respectively; not significantly different from sham). Brain water content, a measure of brain edema, increases from 75.6±0.3% in sham-operated mice to 81.5±0.5% at 24h post-ICH (p<0.05 vs. sham). 6, 12, or 18 mg/kg R-7050 reduces brain water content to 78.5±0.3%, 78.3±0.3%, or 79.3±0.5%, respectively (all treatments p<0.05 vs. ICH; treatments not significantly different from each other). Notably, mice treated with 18 mg/kg exhibit a reduction in general activity/locomotion. As is observed with Evans blue extravasation, R-7050 (6 mg/kg) significantly reduces brain water content after ICH. Administration of R-7050 at 0.5h or 2h post-ICH attenuates brain water content to levels observed in sham-operated mice (p<0.05 vs ICH, not significantly different from sham). |
TNF-α Antagonist III - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.626 ml | 13.131 ml | 26.262 ml |
| 5 mM | 0.525 ml | 2.626 ml | 5.252 ml |
| 10 mM | 0.263 ml | 1.313 ml | 2.626 ml |
| 5 mM | 0.053 ml | 0.263 ml | 0.525 ml |
Last Update：2024-01-02 23:10:35
TNF-α Antagonist III - Reference Information
| biological activity | R-7050 is a cell-permeable TNF-α receptor antagonist, the selectivity for the TNF-α mediated signaling pathway was 2.3-fold higher than for the IL-1β driven signal. |
| Target | Value |
| TNF-α () | 0.63 μM(EC50) |
| IL-1β () | 1.45 μM(EC50) |
Last Update：2024-04-09 15:16:56
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Spot supply
Product Name: R-7050(TNF-α Antagonist III) Visit Supplier Webpage Request for quotationCAS: 303997-35-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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