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化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
2-8°C
生化／生理作用
RIPA-56是一种代谢稳定的III型激酶抑制剂，通过将RIP1锁定在非活性形式，以高效和选择性的方式（RIP1 IC50=13 nM）靶向受体相互作用蛋白1激酶（RIP1；RIPK1），没有抑制作用对RIP3，IDO或一组多种激酶（分别在10、200和5 μM下测试）的效力。RIPA-56可防止培养物中凋亡/NF-κB途径阻断（EC50=27 nM/鼠L929和28 nM/人HT-29细胞）引起的TNFα诱导的坏死病（坏死），以及TNFα诱导的死亡率和多器官体内全身性炎症反应综合征(SIRS)小鼠模型中的损伤（3 mg/kg/12 h或单次6 mg/kg ip的100%存活率），具有良好的药代动力学和生物利用度（10 mg/kg po后）或ip剂量分别为2 mg/kg iv的22%和100%）。据报道，长期每日补充RIPA-56（在食物中为150或300 mg/kg）可防止小鼠衰老相关的雄性生殖系统退化。
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
其他客户在看
Yan Ren et al.
Journal of medicinal chemistry, 60(3), 972-986 (2016-12-20)
On the basis of its essential role in driving inflammation and disease pathology, cell necrosis has gradually been verified as a promising therapeutic target for treating atherosclerosis, systemic inflammatory response syndrome (SIRS), and ischemia injury, among other diseases. Most necrosis
Bo Yan et al.
Chemical communications (Cambridge, England), 53(26), 3637-3640 (2017-03-08)
We report the development of novel Mixed Lineage Kinase Domain-Like protein (MLKL) inhibitors with single nanomolar potency (compound 15 is also named as TC13172). Using the converting biochemistry to chemistry activity-based protein profiling (BTC-ABPP) method, we were able to determine
Dianrong Li et al.
eLife, 6 (2017-08-16)
A pair of kinases, RIPK1 and RIPK3, as well as the RIPK3 substrate MLKL cause a form of programmed necrotic cell death in mammals termed necroptosis. We report here that male reproductive organs of both Ripk3- and Mlkl-knockout mice retain
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