2. Apoptosis MAPK/ERK Pathway Metabolic Enzyme/Protease Immunology/Inflammation
  3. RIP kinase Necroptosis Mixed Lineage Kinase Lactate Dehydrogenase Interleukin Related
  4. RIPK1-IN-38

RIPK1-IN-38 是一种口服有效的 RIPK1 抑制剂，IC50 为 27 nM。RIPK1-IN-38 能抑制 RIPK1 及其下游 RIPK3、MLKL 的磷酸化。RIPK1-IN-38 具有抗坏死性凋亡 (Necroptosis) 的活性。RIPK1-IN-38 在 SIRS 模型和 GVHD 模型中均展现出优异的抗炎活性。RIPK1-IN-38 可用于炎症及免疫相关疾病的研究。

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RIPK1-IN-38

RIPK1-IN-38 Chemical Structure

CAS No. : 3092834-30-2

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RIPK1-IN-38 相关抗体

Top Publications Citing Use of Products

查看 RIP kinase 亚型特异性产品:

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RIPK1 RIPK2 RIPK3

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RIPK1-IN-38 is an orally active RIPK1 inhibitor with an IC50 value of 27 nM. RIPK1-IN-38 can inhibit the phosphorylation of RIPK1 and its downstream signaling molecules RIPK3 and MLKL. RIPK1-IN-38 exhibits anti-necroptotic activity. RIPK1-IN-38 has excellent anti-inflammatory efficacy in both the SIRS model and GVHD model. RIPK1-IN-38 can be used for the research of inflammatory and immune-related diseases[1].

IC50 & Target[1]

RIPK1

27 nM (IC50)

IL-6

 

体外研究
(In Vitro)

RIPK1-IN-38 (Compound 2q) (0.01-10 nM；24 小时) 在 U937、HT-29 和 L929 细胞中可有效阻断 TSZ/TZ 诱导的坏死性凋亡，EC50 分别为 0.75 nM 、0.54 nM 和 0.13 nM[1]。
RIPK1-IN-38 (1.25-5 μM；72 小时) 在 HepG2、LX-2、hPBMC 和 H9c2 细胞中表现出无显著细胞毒性的特性[1]。
RIPK1-IN-38 (30 nM；2 小时) 在 TSZ 处理的 HT-29 细胞中完全抑制了 RIPK1、RIPK3 和 MLKL 的磷酸化[1]。
RIPK1-IN-38 (1.25-5 nM; 9 小时) 在 HT-29 细胞中显著抑制坏死细胞的乳酸脱氢酶 (LDH) 释放[1]。

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

RIPK1-IN-38 相关抗体:

Western Blot Analysis[1]

Cell Line: TSZ-treated HT-29 cells
Concentration: 0.3,3,30,300 nM
Incubation Time: 2,4,6 h
Result: Inhibited the phosphorylation of RIPK1 and its downstream signal proteins RIPK3 and MLKL in a dose- and time-dependent manner.
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice[1] 10 mg/kg i.v. Cmax 4364.87 μg/L
Mice[1] 10 mg/kg p.o. Cmax 2971.36 μg/L
Mice[1] 10 mg/kg i.v. Tmax 0.08 h
Mice[1] 10 mg/kg p.o. Tmax 3.33 h
Mice[1] 10 mg/kg i.v. T1/2 8.63 h
Mice[1] 10 mg/kg p.o. T1/2 10.35 h
Mice[1] 10 mg/kg i.v. CL 0.21 L/h/kg
Mice[1] 10 mg/kg p.o. CL 0.19 L/h/kg
Mice[1] 10 mg/kg i.v. AUC0-t 39926.93 μg/L·h
Mice[1] 10 mg/kg p.o. AUC0-t 42886.31 μg/L·h
Mice[1] 10 mg/kg i.v. V 2.61 L/kg
Mice[1] 10 mg/kg p.o. F 107.41 %
Mice[1] 10 mg/kg p.o. V 2.71 L/kg
体内研究
(In Vivo)

RIPK1-IN-38 (2.5-10 mg/kg，口服，单次) 在 TNFα 诱导的全身炎症反应综合征 (SIRS) 小鼠模型中显著减轻了炎症并提高了存活率[1]。
RIPK1-IN-38 (15-30 mg/kg，口服，第 16-84 天) 在人源化急性移植物抗宿主病 (GVHD) 模型中显著减轻了症状并提高了存活率[1]。

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

Animal Model: C57BL/6 mice (TNF-Induced SIRS model)[1]
Dosage: 2.5 mg/kg, 5 mg/kg, 10 mg/kg
Administration: Oral
Result: Exhibited dose-dependent protection from hypothermia.
Improved mouse survival rate and reduce the level of pro-inflammatory cytokine IL-6 in serum.
Reduced inflammatory damage in the liver and kidneys.
Animal Model: NOG mice transplanted with human PBMCs (humanized acute GVHD model)[1]
Dosage: 15 mg/kg, 30 mg/kg
Administration: Oral
Result: Improved the overall survival rate of mice.
Significantly relieved symptoms such as weak autonomic activity, piloerection, hunchback and weight loss.
Improved colon length and reduced hepatocyte necrosis and periportal lymphocyte infiltration.
分子量

499.56

Formula

C27H22FN5O2S
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

RIPK1-IN-38 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:

RIPK1-IN-383092834-30-2RIP kinaseNecroptosisMixed Lineage KinaseLactate DehydrogenaseInterleukin RelatedReceptor-interacting protein kinasesRIPKMLKsLDHILsystemic inflammatory response syndromeRIPK1 inhibitornecroptosisSIRSGVHDInhibitorinhibitorinhibit

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