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重要文件

SML2100

Sigma-Aldrich

RIPA-56

≥98% (HPLC)

同義詞:

N-苄基-N-羟基-2,2-二甲基丁酰胺, RIPA56

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About This Item

經驗公式(希爾表示法):
C13H19NO2
CAS號碼:
分子量::
221.30
分類程式碼代碼:
12352200
NACRES:
NA.77

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

SMILES 字串

N(O)(Cc1ccccc1)C(=O)C(CC)(C)C

InChI

1S/C13H19NO2/c1-4-13(2,3)12(15)14(16)10-11-8-6-5-7-9-11/h5-9,16H,4,10H2,1-3H3

InChI 密鑰

AVYVHIKSFXVDBG-UHFFFAOYSA-N

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。
高效和选择性受体相互作用蛋白1激酶(RIP1;RIPK1)III型抑制剂,具有抗坏死病的体外和体内功效。

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


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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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