| 中文名称: | R-7050 | ||||
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| 英文名称: | R-7050 | ||||
| 别名: | R 7050 TNF-α Antagonist III | ||||
| CAS No: | 303997-35-5 | 分子式: | C16H8ClF3N4S | 分子量: | 380.77 |
| CAS No: | 303997-35-5 | ||||
| 分子式: | C16H8ClF3N4S | ||||
| 分子量: | 380.77 | ||||
基本信息
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产品编号：R10253 |
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产品名称：R-7050 |
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CAS: |
303997-35-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
380.77 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
9mg/mL warmed with 50ºC water bath (23.63mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内（现配现用） |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.6263mL |
13.1313mL |
26.2626mL |
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5mM |
0.5253mL |
2.6263mL |
5.2525mL |
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10mM |
0.2626mL |
1.3131mL |
2.6263mL |
生物活性
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产品描述 |
一种肿瘤坏死因子受体 (TNFR) 拮抗剂，对 TNFα 具有更高选择性。 |
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靶点/IC50 |
TNF-α |
IL-1β |
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0.63 μM(EC50) |
1.45 μM(EC50) |
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体外研究 |
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 (EC50=0.63μM) is 2- to 3-fold greater than EC50 for IL-1β-induced ICAM-1 expression (EC50=1.45 2μM). 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 molecule (e.g.TRADD,RIP),limits receptor internalization, and prevents subsequent cellular responses after TNF-α binding. |
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体内研究 |
R-7050 (TNF-α Antagonist III) (6 mg/kg) reduces Evans blue extravasation to 28.7±5.9μg and 30.3±1.9 μg Evans blue/g brain tissue when administered at 0.5h or 2h 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 (6mg/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). |
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推荐实验方法(仅供参考)
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动物实验: |
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Mice A mouse collagenase model of ICH is utilized. Briefly, male CD-1 mice (8-10 weeks old) are placed into a stereotactic frame and a 0.5 mm diameter burr hole is drilled over the parietal cortex,2.2mm lateral to the bregma. A 26-gauge Hamilton syringe, loaded with 0.04U of bacterial type IV collagenase in 0.5μL saline, is lowered 3 mm deep from the skull surface directly into the left striatum. The syringe is depressed at a rate of 450nL/min and left in place for several minutes after the procedure to prevent solution reflux and excess diffusion. Sham animals undergo the same surgical procedure, except that saline is stereotactically injected rather than collagenase.After the syringe is removed, bone wax is used to close the burr hole, the incision is surgically stapled, and mice are kept warm until recovery of the righting reflex. R-7050 (6-18mg/kg) is administered via intraperitoneal route at the time of injury or up to 2h post-ICH. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
