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  3. Ferroptosis inducer-7

Ferroptosis inducer-7 是一种口服有效的选择性铁死亡诱导剂,通过作用于肌醇 1,4,5-三磷酸受体(IP3R)/钙释放激活钙通道蛋白 (ORAI) 实现。Ferroptosis inducer-7 在免疫介导的骨髓衰竭中能缓解贫血症状、抑制骨髓 CTL 激活以及改善免疫介导的骨髓衰竭造血功能方面表现出显著作用。Ferroptosis inducer-7 可用于再生障碍性贫血的研究。

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Ferroptosis inducer-7

Ferroptosis inducer-7 Chemical Structure

CAS No. : 2723569-00-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ferroptosis inducer-7 is an orally active and selective ferroptosis inducer via inositol 1,4,5-trisphosphate receptor (IP3R)/calcium release-activated calcium channel protein (ORAI). Ferroptosis inducer-7 exhibits a notable effect in alleviating anemia symptoms, suppressing bone marrow CTLs activation, and improving hematopoietic function in immune-mediated bone marrow failure. Ferroptosis inducer-7 can be studied in research for aplastic anemia[1].

体外研究
(In Vitro)

Ferroptosis inducer-7 (Compound 3a-M1) (1-10 μM) 显著抑制 BALB/c 小鼠淋巴结中 CD8+ T 细胞的增殖以及 IFN-γ 和 TNF-α 的释放[1]
Ferroptosis inducer-7 (7.5-480 μM,72 小时) 与其他免疫细胞系相比,表现出对细胞毒性淋巴细胞系-2 (CTLL-2) 的增殖选择性抑制[1]
Ferroptosis inducer-7 (7.5-30 μM,16 小时) 表明 CTL 功能的抑制是由于用 IL-2 处理的 CTLL-2 中铁死亡的激活所致[1]
Ferroptosis inducer-7 (10 μM,45 分钟) 可增加 CTL 细胞外由 IP3R /ORAI 钙通道触发的Ca2+ 内流[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: IL-2 stimulated CTLL-2 cell line
Concentration: 7.5-30 μM
Incubation Time: 16 h
Result: Showed a significant increase in the phosphorylation levels of mitogen-activated protein kinase, ERK and p38.
Activated the MEK/ERK and p38 MAPK signaling pathway.

Cell Viability Assay[1]

Cell Line: IL-2 stimulated CTLL-2 cell line
Concentration: 7.5-480 μM
Incubation Time: 72 h
Result: Showed the IC50 of Ferroptosis inducer-7 for IL-2-treated CTLL-2 (37.87 μM) was much lower than that for other immune cell lines, such as THP-1 (124.7 μM), HL-60 (132.6 μM), RAW264.7 (491.8 μM), HepG2 (491.9 μM), NRK-52E (705.1 μM), and IEC-6 (84.29 μM).
体内研究
(In Vivo)

Ferroptosis inducer-7 (10 mg/kg,口服,14 天) 不仅对缓解贫血症状、改善造血功能有显著作用,而且在提高免疫介导的骨髓衰竭 BALB/c 小鼠模型的存活率方面也有优势[1]
Ferroptosis inducer-7 (5-15 mg/kg,口服,21 天) 可提高 C57BL/6J 小鼠模型中免疫介导的骨髓衰竭模型的存活率、缓解贫血症状、改善造血功能,尤其是在骨髓衰竭早期阶段[1]
Ferroptosis inducer-7 (5-15 mg/kg,口服,单次给药) 抑制再生障碍性贫血 C57BL/6J 小鼠骨髓中的 T 细胞比例,尤其是 CD8+ 细胞和 CD8+/CD4+ 比率[1]
Ferroptosis inducer-7 (10 g/kg,口服,单次给药) 在小鼠模型中未引起异常,表明最大耐受剂量超过 10 g/kg[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Immune-mediated bone marrow failure BALB/c mice model[1]
Dosage: 10 mg/kg, 14 d
Administration: Oral gavage (p.o.)
Result: Elevated body weight, peripheral red blood cells, hemoglobin levels, and platelet cells in mice.
Improved histopathological changes in the bone marrow, including increased nucleated cells, a restored nucleated-to-red blood cell ratio and a decrease in abnormal proportion of lymphocytes.
Animal Model: Aplastic anemia C57BL/6J mice[1]
Dosage: 5-15 mg/kg, one single dose
Administration: Oral gavage (p.o.)
Result: Reduced the proportion of effector CD8+ T cells, and increased memory CD8+ T cells.
Suppressed the level of IFN-γ and hyperactivation of CTLs in the bone marrow of AA mice.
分子量

489.56

Formula

C29H31NO6

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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Ferroptosis inducer-7
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