2. Apoptosis
  3. RIP kinase Ferroptosis
  4. RIPK1-IN-33

RIPK1-IN-33 是一种具有良好血脑屏障通透性并且具有口服活性的 RIPK1 抑制剂，IC50 为 0.115 μM。RIPK1-IN-33 展现出显著的抗铁死亡 (ferroptosis) 活性、自由基清除能力 (IC50 = 123.3 μM) 以及抗脂质过氧化作用 (IC50 = 9.72 μM)。RIPK1-IN-33 在短暂性大脑中动脉闭塞 (tMCAO) 模型中显著减少脑梗死体积并改善神经功能评分。RIPK1-IN-33 可用于缺血性卒中的研究。

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RIPK1-IN-33

RIPK1-IN-33 Chemical Structure

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RIPK1-IN-33 相关抗体

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查看 RIP kinase 亚型特异性产品:

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RIPK1 RIPK2 RIPK3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RIPK1-IN-33 is a blood-brain barrier-permeable and orally active RIPK1 inhibitor, with an IC50 of 0.115 μM. RIPK1-IN-33 demonstrates remarkable anti-ferroptosis activity, radical scavenging capacity (IC50 = 123.3 μM), and anti-lipid peroxidation effects (IC50 = 9.72 μM). RIPK1-IN-33 markedly reduces cerebral infarction volume and improves neurological function scores in transient middle cerebral artery occlusion (tMCAO) model. RIPK1-IN-33 can be used for the study of ischemic stroke[1].

体外研究
(In Vitro)

RIPK1-IN-33 (Compound 23a) (30-60 min) 展现出显著的自由基清除 DAPH 能力 (IC50 = 123.3 μM) 和抗氧化 MDA 效应 (IC50 = 9.72 μM)[1]。
RIPK1-IN-33 (0.0076-50 μM, 17 h) 在 HT-1080 细胞中以剂量依赖性方式降低 PTGS2 的 mRNA 表达水平 (IC50 = 0.156 μM)[1]。

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

RIPK1-IN-33 相关抗体:

Real Time qPCR[1]

Cell Line: HT-1080 cells
Concentration: 0.0076, 0.0227, 0.0686, 0.206, 0.617, 1.9, 5.6, 16.7, 50 μM
Incubation Time: 17 h
Result: Reduced the mRNA expression level of PTGS2 (IC50 = 0.156 μM) in HT-1080 cells.
Displayed markedly superior anti-ferroptotic activity compared to Edaravone (HY-B0099) (IC50 = 4.92 μM).
体内研究
(In Vivo)

RIPK1-IN-33 (Compound 23a) (33 mg/kg (68.8 μmol/kg)，静脉给药，两次给药，24 h) 在大鼠脑缺血再灌注损伤模型中发挥保护作用[1]。
RIPK1-IN-33 (Compound 23a) (100-200 mg/kg，静脉给药，单次给药或每日一次持续 7 天) 在大鼠脑缺血再灌注损伤模型中未出现死亡或严重不良事件[1]。

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

Animal Model: Adult male Sprague-Dawley rats (200-230 g) subjected to transient middle cerebral artery occlusion (tMCAO)[1]
Dosage: 33 mg/kg (68.8 μmol/kg)
Administration: i.v. for twice doses and the second dose was administered 6 h later
Result: Reduced infarct volume in tMCAO rats compared to the vehicle control.
Improved neurological function in tMCAO rats.
Downregulated MDA level.
Reduced the protein expression of necroptosis-associated caspase-3 in the ischemic penumbra.
Downregulated the protein expression of cyclooxygenase-2 (COX-2, encoded by PTGS2).
Upregulated glutathione peroxidase 4 (GPX4) within the ferroptosis pathway.
Animal Model: Adult male Sprague-Dawley rats (200-230 g) subjected to transient middle cerebral artery occlusion (tMCAO)[1]
Dosage: 100, 200 mg/kg
Administration: i.v. for a single dose or i.v. once daily for 7 days
Result: Showed no abnormalities in body weight, food consumption, organ-to-body weight ratios, blood biochemical parameters, or gross necropsy findings.
分子量

479.52

Formula

C26H27F2N5O2
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

RIPK1-IN-33 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RIPK1-IN-33RIP kinaseFerroptosisReceptor-interacting protein kinasesRIPKRIPK1ischemic stroketMCAOferroptosisInhibitorinhibitorinhibit

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