2. Metabolic Enzyme/Protease Neuronal Signaling NF-κB Immunology/Inflammation Apoptosis
  3. Lipoxygenase Amyloid-β Reactive Oxygen Species (ROS) Apoptosis
  4. CNB-001

CNB-001 是一种强效且具有口服活性的 5-脂氧合酶 (5-LOX) 抑制剂。CNB-001 可降低 5-LOX 的表达并提高蛋白酶体活性。CNB-001 能抑制可溶性 Amyloid-β 和泛素化聚集蛋白的积累。CNB-001 可抑制凋亡 (apoptosis)、活性氧 (ROS) 的产生，并稳定线粒体膜电位。CNB-001 能够减轻胰岛素抵抗并增加葡萄糖摄取。CNB-001 还具有抗缺血和抗炎作用。CNB-001 可用于炎症、神经系统和代谢性疾病的研究，如阿尔茨海默病、中风和糖尿病。

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CNB-001

CNB-001 Chemical Structure

CAS No. : 1019110-87-2

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100 mg ￥200
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CNB-001 相关抗体

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5-LOX 12-LOX 15-LOX

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CNB-001 is a potent and orally active 5-lipoxygenase (5-LOX) inhibitor. CNB-001 can decreases 5-LOX expression and increase proteasome activity. CNB-001 can inhibit accumulation of soluble Amyloid-β and ubiquitinated aggregated proteins. CNB-001 can inhibit apoptosis, ROS production and stabilize mitochondrial membrane potential. CNB-001 can reduce insulin resistance and increase glucose uptake. CNB-001 also exhibits anti-ischemic, anti-inflammatory effects. CNB-001 can be used for the researches of inflammation, neurological and metabolic disease, such as Alzheimer's disease, stroke and diabetes[1][2][3][4].

IC50 & Target[1][2]

5-LOX

70 nM (IC50)

15-LOX

 

体外研究
(In Vitro)

CNB-001 (1 μM, 24-96 h) 可抑制 MC65 细胞中 Aβ 聚集并促进其清除[1]。
CNB-001 (1 μM, 48 h) 可激活 MC65 细胞中的三种蛋白酶体活性 (胰凝乳蛋白酶样、胰蛋白酶样、半胱天冬酶样) 并降解 Aβ[1]。
CNB-001 (1 μM, 1-24 h) 可诱导 MC65 细胞中 eIF2α (Ser51) 磷酸化并增加 ATF4 的表达[1]。
CNB-001 (1 μM, 1-24 h) 可抑制 5-脂氧合酶 (5-LOX，IC50 值为 70 nM)，并增加 MC65 细胞中 5-LOX 的 S523 磷酸化，降低其 S271 磷酸化[1]。
CNB-001 可抑制人外周血单个核淋巴细胞 (PBML) 中白三烯 B4 (LTB4) 的产生，IC50 值为 0.076 μM[2]。
CNB-001 (0-2 μM) 可抑制兔网织红细胞中的 15-脂氧合酶[2]。
NB-001 (0.5-15 μM, 24 h) 在静止的 C2C12 肌管中的半数毒性浓度 (TC50) 为 15.3 μM[3]。
CNB-001 (1 μM, 12 h) 可逆转棕榈酸 (HY-N0830) 诱导的胰岛素抵抗，并恢复 C2C12 肌管中胰岛素刺激的葡萄糖摄取[3]。
CNB-001 通过抑制细胞内活性氧的产生、凋亡以及稳定线粒体膜电位，保护 SK-N-SH 人神经母细胞瘤细胞免受 Rotenone (HY-B1756) 诱导的神经毒性[4]。

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

CNB-001 相关抗体:

Western Blot Analysis[1]

Cell Line: MC65 cells
Concentration: 1 μM
Incubation Time: 1, 2, 4 and 6 h
Result: Increased S523 phosphorylation and decreases S271 phosphorylation of 5-LOX.
体内研究
(In Vivo)

CNB-001 (25 mg/kg diet，口服，每日一次，持续 6 个月) 可改善 APPswe/PS1E9 转基因小鼠的工作记忆[1]。
CNB-001 (500 mg/kg，口服，在注射 Aβ1-42 前 30 分钟给药) 可完全逆转注射 Aβ1-42 小鼠的情境记忆损伤[1]。
CNB-001 (5-50 mg/kg，静脉注射，栓塞后 5 或 60 分钟) 可改善新西兰白兔栓塞性中风的行为缺陷[2]。
CNB-001 (10 mg/kg，静脉注射，大脑中动脉闭塞后 5 分钟) 可减少恒河猴永久性大脑中动脉闭塞 (MCAO) 的梗死扩大[2]。
CNB-001 (40 mg/kg，腹腔注射，每日一次，周末除外，持续 20-22 周) 可减轻高脂饮食诱导的 C57BL/6J 小鼠肥胖和胰岛素抵抗[3]。
CNB-001 (24 mg/kg，腹腔注射，从第 1 天到第 7 天每日一次) 可减轻 MPTP 诱导的帕金森病 (PD) 小鼠的运动障碍和神经毒性[4]。

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

Animal Model: APPswe/PS1E9 transgenic models[1]
Dosage: 25 mg/kg diet
Administration: Orally administration, daily for 6 months
Result: Increased arm alternation choices.
Increased eIF2α phosphorylation, ATF4 and HSP90 expression in the hippocampus.
Reduced soluble Aβ1-42 (50%) and ubiquitinated aggregated proteins.
Increased the expression of synapse-associated proteins (phosphorylated synapsin-1, Pro-BDNF, Homer1).
Decreased the expression of clusterin and 5-LOX (>40%).
Animal Model: New Zealand white rabbits with embolic stroke[2]
Dosage: 5-50 mg/kg 1 h post-embolization and 10 mg/kg 5 min post-embolization
Administration: Intravenously injection
Result: Increased P50 (clot burden causing 50% neurological dysfunction) by 74%.
Decreased COX-2 and 5-LOX expression, and increased BDNF levels in ipsilateral cortical tissues.
Animal Model: High-fat diet-induced obesity and insulin resistance in C57BL/6J mice models[3]
Dosage: 40 mg/kg
Administration: Intraperitoneally injection, daily except weekends for 20-22 weeks
Result: Reduced body weight gain (without altering food intake).
Decreased serum triglyceride and interleukin-6 (IL-6) levels.
Improved glucose tolerance (lowers IPGTT AUC) and insulin sensitivity (lowers IPITT AUC).
Restored insulin-stimulated glucose uptake in gastrocnemius muscle.
Upregulated insulin signaling molecules (p-IR, p-Akt) and downregulates protein-tyrosine phosphatase 1B (PTP1B) and phospho-eIF2α in skeletal muscle.
Attenuated hepatic steatosis (reduces liver triglycerides and Oil Red O-stained fat droplets), and increased energy expenditure (without changing respiratory exchange ratio, RER).
Animal Model: MPTP-induced Parkinson’s disease (PD) mice[4]
Dosage: 24 mg/kg
Administration: Intraperitoneally injection, daily from day 1 to day 7
Result: Reduced runway crossing time and foot slip errors in the narrow beam test.
Shortened fixed posture duration and reduced latency to shift four limbs.
Restored striatal dopamineand its metabolites (DOPAC, HVA) levels.
Decreased nitrite and citrulline accumulation.
Downregulated pro-inflammatory factors (TNF-α, IL-1β, IL-6, iNOS, GFAP, COX-2) and pro-apoptotic markers (Bax, cytochrome C, cleaved caspase-3).
Upregulated anti-apoptotic Bcl-2, and increased dopamine transporter (DAT) immunoreactivity in the substantia nigra (SN) and striatum (ST).
分子量

440.49

Formula

C27H24N2O4
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

纯度 & 产品资料
参考文献

CNB-001 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)

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

CNB-0011019110-87-2CNB001CNB 001LipoxygenaseAmyloid-βReactive Oxygen Species (ROS)ApoptosisLOXβ-amyloid peptideAβAbeta5-LOXROSMitochondrial membrane potentialInsulin resistanceAlzheimer's diseaseParkinson diseaseDiabetesNeuroinflammationInhibitorinhibitorinhibit

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