2. Apoptosis
  3. RIP kinase Necroptosis
  4. RIP1-IN-1

RIP1-IN-1 是一种口服有效的 RIP1 抑制剂，具有很强的 RIP1 结合亲和力 (Kd：110 nM)。RIP1-IN-1 表现出很强的抗坏死性凋亡 (Necroptosis) 活性。RIP1-IN-1 通过阻断 RIP1、RIP3 和 MLKL 信号通路的磷酸化有效抑制坏死小体的形成。RIP1-IN-1 可抑制坏死性凋亡，可用于急性肝损伤的研究。

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RIP1-IN-1 Chemical Structure

RIP1-IN-1 Chemical Structure

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RIP1-IN-1 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

RIP1-IN-1 is an orally active RIP1 inhibitor with strong RIP1 binding affinity (Kd: 110 nM). RIP1-IN-1 exhibits strong anti-necroptosis activity. RIP1-IN-1 effectively inhibits the formation of necrosomes by blocking the phosphorylation of RIP1, RIP3 and MLKL signaling pathways. RIP1-IN-1 inhibits necroptosis and can be used in the study of acute liver injury[1].

IC50 & Target[1]

RIPK1

110 nM (Kd)

体外研究
(In Vitro)

RIP1-IN-1 (Compound N-1) (0-1.6 μM，5-24h) 可以有效且剂量依赖性地抑制 Z-VAD-FMK (HY-16658B) 诱导的 HT-29 细胞坏死性凋亡，以及 Z-VAD-FMK (HY-16658B) 诱导的 U937 细胞坏死性凋亡[1]。
RIP1-IN-1 在 HT-29 细胞中表现出强效的抗坏死性凋亡活性 (CC50：>50 μM, EC50：8.8 nM)[1]。
RIP1-IN-1 (0.4 μM，2-6 h) 有效抑制 Z-VAD-FMK (HY-16658B) 处理的 HT-29 细胞中 RIP1 和 RIP3 的磷酸化，具有时间依赖性，从而抑制下游靶标 MLKL 的磷酸化[1]。
RIP1-IN-1 (0.097-400 nM 5h) 剂量依赖性抑制 RIP1/3 和 MLKL 的磷酸化[1]。
RIP1-IN-1 (400 nM, 6 h) 在 HT-29 细胞中通过阻断 RIP1/RIP3/MLKL 通路的磷酸化来抑制 Z-VAD-FMK 诱导的坏死小体形成，从而显示其抗坏死凋亡活性[1]。

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

RIP1-IN-1 相关抗体:

Western Blot Analysis[1]

Cell Line: Z-VAD-FMK (30 μM) treated HT-29 cells
Concentration: 0.097、1.562、25、400 nM
Incubation Time: 2-6 h
Result: Prevented the phosphorylation of both RIP1 and RIP3 within 2-6 h and subsequently inhibited downstream target MLKL phosphorylation.
Reduced pRIP1, pRIP3, and pMLKL levels in a dose-dependent manner in the range of 0.097-400 nM.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Rat 10 mg/kg i.g. T1/2 0.82 hr
Rat 10 mg/kg i.g. Tmax 0.5 hr
Rat 10 mg/kg i.g. Cmax 726 ng/mL
Rat 10 mg/kg i.g. MRT 1.65 hr
Rat 10 mg/kg i.g. CL/F 116 mL/min/kg
Rat 10 mg/kg i.g. Vd/F 8.29 L/kg
Rat 10 mg/kg i.g. AUC0-t 1.442 μg·h/mL
Rat 10 mg/kg i.g. AUC0-inf 1.449 μg·h/mL
Rat 10 mg/kg i.g. F 26.3 %
体内研究
(In Vivo)

RIP1-IN-1 (Compound N-1) (1、3、5 mg/kg，口服) 在 SIRS (全身炎症反应综合征) 小鼠中表现出抗坏死凋亡作用[1]。
RIP1-IN-1 (3 mg/kg，口服，每天一次，连续 14 天) 在 CCl4 诱发的小鼠急性肝损伤模型中表现出对急性肝损伤的保护作用[1]
RIP1-IN-1 (10 mg/kg，口服) 在 Sprague-Dawley 大鼠中表现出短的半衰期和高的清除率[1]。

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

Animal Model: C57BL/6 mice; Establishment of SIRS mice model by combining mTNF-α (65 μg/kg) and Z-VAD-FMK (200 μg/piece)[1]
Dosage: 1, 3, 5 mg/kg (5 % DMSO and 95 % CMC-Na solution)
Administration: p.o.
Result: Significantly improved the survival rate of SIRS mice, reaching 20%, 50% and 90%.
Alleviated mTNF-α-induced hypothermia within 9 hours.
Significantly reduced serum IL-6 levels, indicating its anti-inflammatory effect.
Animal Model: Male ICR mice (6-8 weeks old), 0.01 % CCl4 induced acute liver injury mice model[1]
Dosage: 1, 3, 5 mg/kg (5 % DMSO and 95 % CMC-Na solution)
Administration: i.g., once daily for 14 consecutive days
Result: Significantly reduced RIP1, RIP3, and MLKL phosphorylation in diseased mice, thereby restoring AST and ALT markers indicative of liver damage.
HE staining showed that the liver tissue structure was close to normal at a dose of 3mg/kg and 5mg/kg, and the damage was significantly reduced.
The result showed that ALT, AST, and IL-6 levels were significantly reduced and close to the normal range, indicating that it can play a protective role against acute liver damage.
Western Blot results showed that it can effectively inhibit phosphorylation and block the necroptosis pathway.
分子量

423.46

Formula

C26H21N3O3
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

RIP1-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

RIP1-IN-1RIP kinaseNecroptosisReceptor-interacting protein kinasesRIPKRIP1 inhibitoracute liver injurySIRSphosphorylation inhibitionRIP1/RIP3/MLKL pathwayInhibitorinhibitorinhibit

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