NecroX-7 是一种有效的自由基清除剂和HMGB1(高迁移率族蛋白 1) 抑制剂。NecroX-7 可以作为对乙酰氨基酚毒性的解毒剂。NecroX-7 通过抑制缺血/再灌注损伤中 HMGB1 的释放发挥保护作用。NecroX-7 抑制 HMGB1 诱导的TNF和IL-6的释放,以及TLR-4和晚期糖基化终产物受体的表达,用于移植物抗宿主病 (GVHD) 研究。
产品描述
NecroX-7 is a potent free radical scavenger and a HMGB1 (high-mobility group box 1) inhibitor. NecroX-7 can be used as an antidote to acetaminophen toxicity. NecroX-7 exerts a protective effect by preventing the release of HMGB1 in ischemia/reperfusion injury. Additionally, NecroX-7 inhibits the HMGB1-induced release of TNF and IL-6, as well as the expression of TLR-4 and receptor for advanced glycation end products. NecroX-7 may be use for treatment of graft-versus-host disease (GVHD) research [1].
体外活性
NecroX-7 (0-40 μM, 3-4 d) inhibits activated or proliferating T cells without causing apoptosis [1]. NecroX-7 (0-40 μM) significantly lowers HMGB1 levels in a dose-dependent manner [1]. NecroX-7 inhibits formation of mitochondria-specific ROS/reactive nitrogen species in H9C2 cells and hepatocytes after induction by tert-butyl hydroperoxide or doxorubicin [1]. NecroX-7 increased regulatory T cell numbers, which may be associated with regulation of differentiation signals independent of HMGB1 [1]. Cell Proliferation Assay [1] Cell Line: CD4 T cells Concentration: 0, 0.625, 1.25, 2.5, 5, 10, 20, and 40 μM Incubation Time: 3-4 d Result: Showed a marked reduction in splenocyte proliferation, in a dose-dependent manner. Modulated alloreactive T cell responses.
体内活性
NecroX-7 (0-0.3 mg/kg, IV, once injection at 2-d intervals, for 2 weeks) markedly reduces GVHD-related mortality and inhibits severe tissue damage [1]. NecroX-7 protects mice against lethal GVHD by reciprocal regulation of regulatory T/Th1 cells, attenuating systemic HMGB1 accumulation and inhibiting HMGB1-mediated inflammatory response [1]. Animal Model: Female BALB/c and C57BL/6 mice (Eight-week-old, with GVHD) [1] Dosage: 0.03, 0.1, and 0.3 mg/kg Administration: IV, once injection at 2-d intervals, for 2 weeks Result: Observed statistically significant prolonged survival at doses ≥0.1 mg/kg: 30–60% of mice in these treatment groups survived for >50 d. Significantly improved clinical signs and prolonged survival, and the mice showed a reduction in clinical manifestations of acute GVHD, including weight loss, hunched posture, diarrhea, and ruffled fur.
Cas No.
1120332-55-9
分子式
C24H29N3O3S
分子量
439.57
别名
LC28-0126;LC28 0126;LC-280126
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years