303997-35-5
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- CAS号:
- 303997-35-5
- 英文名:
- R-7050
- 英文别名:
- R-7050;R-7050;R 7050;R7050;TNF-α Antagonist III;TNF-α Antagonist III;TNF-alpha Antagonist III, R-7050;8-Chloro-4-(phenylthio)-1-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]quinoxaline;[1,2,4]Triazolo[4,3-a]quinoxaline, 8-chloro-4-(phenylthio)-1-(trifluoromethyl)-;R 7050,Inhibitor,R7050,inhibit,TNFR,Tumor Necrosis Factor Receptor,TNF Receptor,R-7050
- 中文名:
- 303997-35-5
- 中文别名:
- 化合物R-7050;R 7050,TNF-Α受体信号拮抗剂;8-氯-4-(苯硫基)-1-(三氟甲基)-[1,2,4]三唑并[4,3-A]喹喔啉
- CBNumber:
- CB53152725
- 分子式:
- C16H8ClF3N4S
- 分子量:
- 380.77
- MOL File:
- 303997-35-5.mol
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303997-35-5化学性质
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密度:
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1.59±0.1 g/cm3(Predicted)
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储存条件:
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Sealed in dry,Store in freezer, under -20°C
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溶解度:
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insoluble in H2O; ≥17.67 mg/mL in DMSO; ≥2.2 mg/mL in EtOH with gentle warming and ultrasonic
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形态:
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crystalline solid
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酸度系数(pKa):
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-3.70±0.30(Predicted)
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303997-35-5性质、用途与生产工艺
R-7050是一种具有细胞透性的TNF-α受体拮抗剂,对TNF-α所介导的信号通路的选择性是对IL-1β驱动的信号的2.3倍。
Target | Value |
TNF-α
()
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0.63 μM(EC50)
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IL-1β
()
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1.45 μM(EC50)
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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.
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).
303997-35-5
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上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-110203 | R-7050 | | 1 mg | 340元 |
2024/04/30 | HY-110203 | 303997-35-5 R-7050 | 303997-35-5 | 5mg | 750元 |
303997-35-5, 303997-35-5 相关搜索:
- 药靶配体
- R 7050,TNF-Α受体信号拮抗剂
- 8-氯-4-(苯硫基)-1-(三氟甲基)-[1,2,4]三唑并[4,3-A]喹喔啉
- 化合物R-7050
- 303997-35-5
- R 7050,Inhibitor,R7050,inhibit,TNFR,Tumor Necrosis Factor Receptor,TNF Receptor,R-7050
- TNF-α Antagonist III
- TNF-alpha Antagonist III, R-7050
- [1,2,4]Triazolo[4,3-a]quinoxaline, 8-chloro-4-(phenylthio)-1-(trifluoromethyl)-
- TNF-α Antagonist III
- 8-Chloro-4-(phenylthio)-1-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]quinoxaline
- R-7050;R 7050;R7050
- R-7050