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R-7050  ≥98%

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（25 mg/mL 超声）
产品描述：基本信息 产品编号：R10253 产品名称：R-7050 CAS: 303997-35-5   储存条件 粉末 -20℃ 四年     分子式： C16H8ClF3N4S 溶于液体 -80℃ 六个月 分子量 380.77 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 9mg/mL warmed with 50ºC water bath (23.63mM) Ethanol Insoluble Water Insoluble 体内（现配现用）     ＜1mg/ml表示微溶或不溶。 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。 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.6263mL 13.1313mL 26.2626mL 5mM 0.5253mL 2.6263mL 5.2525mL 10mM 0.2626mL 1.3131mL 2.6263mL   生物活性 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。 靶点/IC50 TNF-α IL-1β  0.63 μM(EC50) 1.45 μM(EC50) 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. 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).   推荐实验方法(仅供参考)   动物实验:   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.
保存条件：-20℃

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