2. Immunology/Inflammation Metabolic Enzyme/Protease
  3. NOD-like Receptor (NLR) Interleukin Related Cytochrome P450
  4. NT-0527

NT-0527是一种具有选择性、口服活性、血脑屏障穿透性的 NLRP3 炎症小体 (NLRP3 inflammasome) 抑制剂。NT-0527 可特异性阻断 NLRP3 炎症小体的形成，从而减少 IL-1β 的成熟和释放，并抑制 CYP2C19 的活性。NT-0527 在小鼠 LPS (HY-D1056) /ATP (HY-B2176) 诱导的腹膜炎模型中显示出抗炎活性。NT-0527 可用于研究与 NLRP3 炎症小体相关的神经炎症性疾病 (帕金森病、阿尔茨海默病、肌萎缩侧索硬化症) 和外周炎症性疾病 (II 型糖尿病、动脉粥样硬化、痛风等) 。

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NT-0527

NT-0527 Chemical Structure

CAS No. : 2771019-10-2

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规格 价格 是否有货 数量
5 mg ￥405
In-stock
10 mg ￥630
In-stock
25 mg ￥1215
In-stock
50 mg ￥1935
In-stock
100 mg ￥3060
In-stock
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Customer Review

NT-0527 相关抗体

Top Publications Citing Use of Products

查看 NOD-like Receptor (NLR) 亚型特异性产品:

查看所有亚型
NLRP3 NLRP1 NOD1 NOD2

查看 Interleukin Related 亚型特异性产品:

查看所有亚型
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

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NT-0527 is a selective, orally active, and brain-permeable NLRP3 inflammasome inhibitor. NT-0527 can specifically block the formation of the NLRP3 inflammasome, resulting in the reduction in the maturation and release of IL-1β, exhibit inhibition on CYP2C19. NT-0527 displays anti-inflammatory activity in the mouse LPS (HY-D1056) /ATP (HY-B2176)-induced peritonitis model. NT-0527 can be used for the research of neuroinflammatory disorders (Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis) and peripheral inflammatory disorders (type II diabetes, atherosclerosis, gout, etc.) associated with NLRP3 inflammasome[1].

IC50 & Target

IL-1β

0.79 μM (IC50)

CYP2C19

 

NLRP3 inflammasome

 

体外研究
(In Vitro)

NT-0527 (0.001-10 μM; 90 min) 在人外周血单核细胞中以剂量依赖的方式破坏 NLRP3 炎症小体的形成并减少 IL-1β 的释放，ATP、MSU和CPPD 刺激的 IC50 值分别为 0.062 μM、0.087 μM 和 0.040 μM[1]。
NT-0527 (0.01-100 μM; 3.5 h) 在人全血中以剂量依赖的方式抑制 IL-1β 的产生，平均 IC50 为 0.79 μM，且具有高度选择性，对 IL-6 和 TNFα 的释放无显著影响[1]。
NT-0527 (250 nM, 1 μM; 30 min) 在人外周血单核细胞中显著抑制 NLRP3 介导的 IL-1β 释放，是一种特异性 NLRP3 抑制剂[1]。
NT-0527 (5 μM) 在 Caco-2 单层细胞模型中表现出较高的被动渗透性和外排率，且不是外排转运蛋白的底物[1]。
NT-0527 (1 μM) 在人肝微粒体和冷冻保存的肝细胞中显示出极低的固有清除率，而在大鼠和小鼠肝微粒体和冷冻保存的肝细胞中显示出中等至高的固有清除率，表明其在人肝脏中的代谢清除率远低于大鼠和小[1]。

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

NT-0527 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route MRT CLplasma Vss AUC0-inf F
Cynomolgus Monkey[1] 3 mg/kg i.v. 3.9 h 6.3 mL/min/kg 1.4 L/kg 8200 ng·h/mL 104 %
Cynomolgus Monkey[1] 3 mg/kg p.o. 3.9 h 6.3 mL/min/kg 1.4 L/kg 9700 ng·h/mL 104 %
Mice[1] 3 mg/kg i.v. 0.25 h 42 mL/min/kg 0.63 L/kg 1200 ng·h/mL 39 %
Mice[1] 3 mg/kg p.o. 0.25 h 42 mL/min/kg 0.63 L/kg 470 ng·h/mL 39 %
Pig[1] 1 mg/kg i.v. / / / / /
Pig[1] 2 mg/kg p.o. / / / / /
Rat[1] 3 mg/kg i.v. 0.58 h 10 mL/min/kg 0.36 L/kg 4800 ng·h/mL 50 %
Rat[1] 3 mg/kg p.o. 0.58 h 10 mL/min/kg 0.36 L/kg 2400 ng·h/mL 50 %
体内研究
(In Vivo)

NT-0527 (5 μM；颈动脉灌注；0.25-0.5 min) 在雄性 SD 大鼠原位脑灌注模型中表现出较高的脑通透性[1]。 NT-0527 (10 mg/kg；灌胃；单次给药；24 h) 在血液和脑脊液中几乎均匀分布[1]。 NT-0527 (1-100 mg/kg；灌胃) 呈剂量依赖性地抑制腹膜 IL-1β 的产生，在 10 mg/kg 时效果显著[1]。

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

Animal Model: Male non-naïve cynomolgus monkeys were administered formulated in 0.5 % methocel (400cp) and 0.2 % Tween 80 in purified water[1].
Dosage: 10 mg/kg
Administration: Oral gavage (p.o.); single administration; 24 h
Result: Achieved an almost even distribution between blood and cerebrospinal fluid (CSF), demonstrating efficient central nervous system (CNS) penetration.
Animal Model: Male SD rats (fed) were subjected to non-recovery anaesthesia and cannulated at the right carotid artery for hemi-brain perfusion[1].
Dosage: 5 μM
Administration: Carotid artery perfusion; single administration; 0.25-0.5 min
Result: Exhibited high brain permeability, which was significantly higher than the low-permeability sulfonylurea NLRP3 inhibitors CRID3 (0.09 μM) (HY-12815) and emlenoflast (0.25 μM) (HY-137245); the permeability was higher than the high-permeability control diazepam (4.3 μM).
分子量

360.77

Formula

C17H14ClFN4O2
CAS 号
性状

固体

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

NT-0527 相关分类

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  • 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:

NT-05272771019-10-2NT0527NT 0527NOD-like Receptor (NLR)Interleukin RelatedCytochrome P450ILCYPsNLRP3 inflammasome inhibitorinhibition of IL-1β releaseinhibition of CYP2C19human peripheral blood mononuclear cells (PBMCs)human whole bloodCaco-2 monolayer cellsC57BL/6J miceSD ratscynomolgus monkeysBama minipigsmouse LPS/ATP-induced peritonitis modelrat in situ brain perfusion modelcynomolgus monkey CSF exposure modelParkinson's diseaseAlzheimer's diseaseamyotrophic lateral sclerosis (ALS)type II diabetesatherosclerosisobesitygoutasthmainflammatory bowel disease (IBD)Metabolic DiseaseInhibitorinhibitorinhibit

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