2. Immunology/Inflammation NF-κB Apoptosis
  3. Toll-like Receptor (TLR) NO Synthase NF-κB TNF Receptor Interleukin Related
  4. CIAC101

CIAC101 是一种有效的且可透过血脑屏障的 TLR4 抑制剂，其 IC50 值为 17.0 nM 。CIAC101 可阻断 Lipopolysaccharides (HY-D1056) (LPS) 诱导的 NF-κB 激活，并降低促炎介质 (iNOS、IL-1β、TNF-α 和 IL-6) 的表达。CIAC101 具有强大的抗神经炎症活性和对抗药物诱发的神经行为适应的效果。CIAC101 可用于成瘾和神经疾病的研究。

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CIAC101

CIAC101 Chemical Structure

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Customer Review

CIAC101 相关抗体

Top Publications Citing Use of Products

查看 Toll-like Receptor (TLR) 亚型特异性产品:

查看所有亚型
TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

查看 NO Synthase 亚型特异性产品:

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nNOS iNOS eNOS

查看 NF-κB 亚型特异性产品:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 TNF Receptor 亚型特异性产品:

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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

CIAC101 is a potent and brain-penetrant TLR4 antagonist with an IC50 of 17.0 nM in NO assay. CIAC101 blocks Lipopolysaccharides (HY-D1056) (LPS)-induced NF-κB activation and reduces the expression of pro-inflammatory mediators (iNOS, IL-1β, TNF-α, and IL-6). CIAC101 robust antineuroinflammatory activity with efficacy against drug-evoked neurobehavioral adaptations. CIAC101 can be used for the research of addiction and neurological disease[1].

IC50 & Target[1]

TLR4

17 nM (IC50)

NF-κB

 

iNOS

 

TNF-α

 

IL-1β

 

IL-6

 

体外研究
(In Vitro)

CIAC101 抑制 Lipopolysaccharides (HY-D1056) (LPS) 诱导的小胶质细胞 BV-2 中 NO 的过度产生，IC50 值为 17 nM[1]。
CIAC101 (0.1 nM-10 μM；24 h) 呈剂量依赖性地抑制 LPS 诱导的 NF-κB 活化 (IC50 为 65.5 nM)，并降低 HEK-BluehTLR4 细胞中促炎介质的表达。CIAC101 未显示明显的细胞毒性[1]。
在 BV-2 NF-κB 荧光素酶报告细胞系中，CIAC101 (0.1 nM-10 μM；24 h) 呈剂量依赖性地抑制 LPS 诱导的 NF-κB 活化，且未显示明显的细胞毒性，IC50 为 90.2 nM[1]。
在 LPS 刺激的 BV-2 小胶质细胞模型中，CIAC101 (0.01-1 μM；24 h) 以浓度依赖的方式降低 LPS 诱导的 iNOS、IL-1β、TNF-α 和 IL-6 的 mRNA 表达[1]。

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

CIAC101 相关抗体:

RT-PCR[1]

Cell Line: BV-2 microglial were treated with 200 ng/mL LPS
Concentration: 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 24 h
Result: Reduced LPS-evoked mRNA expression of iNOS, IL-1β, TNF-α, and IL-6.
体内研究
(In Vivo)

CIAC101 (0.005-0.2 mg/kg，腹腔注射，第 4 天至第 10 天) 能有效对抗甲基苯丙胺 (METH) 引发的小鼠 (Balb/c) 神经行为适应性变化和神经炎症[1]。
CIAC101 (20 mg/kg；腹腔注射；每日一次；持续 14 天) 在 Balb/c 小鼠中耐受性良好，未见急性全身或器官毒性。

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

Animal Model: Male Balb/c mice (6-8 weeks; 22-25 g) (METH-induced neuroinflammation and addiction-like behaviors)[1]
Dosage: 0.005 mg/kg, 0.02 mg/kg, 0.2 mg/kg
Administration: Intraperitoneal (i.p.)
Result: Significantly reduced METH-induced behavioral sensitization and conditioned place preference (CPP).
Also attenuated microglial activation and proinflammatory gene expression (IL-1β, TNF-α, and IL-6) in the medial prefrontal cortex (mPFC) and ventral tegmental area (VTA).
分子量

395.49

Formula

C24H29NO4
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

CIAC101 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 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

CIAC101CIAC 101CIAC-101Toll-like Receptor (TLR)NO SynthaseNF-κBTNF ReceptorInterleukin RelatedNitric oxide synthasesNOSNuclear factor-κBNuclear factor-kappaBTumor Necrosis Factor ReceptorTNFRILareacortexmethamphetamineaddictionsensitizationBV-2prefrontaltegmentalMETHconditionedantineuroinflammatoryneuroimmunemicrogliapreferencemedialplaceTLR4ventralbehavioralInhibitorinhibitorinhibit

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