2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. Adrenergic Receptor Calcium Channel Potassium Channel Reactive Oxygen Species (ROS)
  4. Landiolol

Landiolol (ONO1101) 是一种高选择性的超短效 β1 肾上腺素受体竞争性抑制剂。Landiolol 特异性阻断心脏 β1 受体，降低心率和心肌耗氧量。Landiolol 在脓毒症模型中抑制 TNF-α 诱导的线粒体过度氧消耗和活性氧 (ROS) 生成，减轻肾损伤。Landiolol 对心脏离子通道 (如 L 型钙电流、内向整流钾电流) 影响甚微，负性肌力作用较弱。Landiolol 可用于围手术期心动过速控制、脓毒症相关急性肾损伤的保护研究。

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Landiolol Chemical Structure

Landiolol Chemical Structure

CAS No. : 133242-30-5

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Landiolol 的其他形式现货产品:

Customer Review

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Landiolol 相关抗体

Top Publications Citing Use of Products

查看 Adrenergic Receptor 亚型特异性产品:

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α adrenergic receptor β adrenergic receptor

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Landiolol (ONO1101) is a highly selective, ultra-short-acting competitive inhibitor of β1 adrenergic receptors. Landiolol specifically blocks cardiac β1 receptors, reducing heart rate and myocardial oxygen consumption. Landiolol inhibits TNF-α-induced excessive mitochondrial oxygen consumption and reactive oxygen species production in a sepsis model, alleviating renal injury. Landiolol has little effect on cardiac ion channels (such as L-type calcium current and inward rectifier potassium current) and has a weak negative inotropic effect. Landiolol can be used for perioperative tachycardia control and protection studies of sepsis-related acute kidney injury[1][2][3].

IC50 & Target

Beta-1 adrenergic receptor

 

L-type calcium channel

 

IrK

 

体外研究
(In Vitro)

Landiolol (10 μM；24 h) 显著抑制 HEK293 细胞中 TNF-α (0.5 nM) 诱导的线粒体氧消耗率 (OCR) 升高，使基础 OCR 从 123% 降至 94.8%，并减少活性氧 (ROS) 生成[1]。
Landiolol (10 μM；24 h) 抑制 TNF-α (0.5 nM) 诱导的 HEK293 细胞的过度糖酵解能力，但不显著影响其基础糖酵解 (ECAR) 水平[1]。

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

Landiolol 相关抗体:

Cell Viability Assay[1]

Cell Line: HEK293 cells
Concentration: 10 μM (Landiolol)
Incubation Time: 24 h; with 0.5 nM TNF-α
Result: Resulted in a significant reduction in basal OCR compared to TNF-α alone. The OCR, normalized to control (100%), decreased from 123.9%±16.6% (TNF-α only) to 94.8%±13.3% (TNF-α + Landiolol).
Attenuated maximal OCR and ATP production, indicating inhibition of mitochondrial hyperactivity.
Significantly lowered intracellular ROS levels, measured via dichlorodihydrofluorescein (DCF) assay.
体内研究
(In Vivo)

Landiolol (0.1 mg/kg/min；静脉输注；单剂量；6 h) 显著降低脂多糖 (LPS) 诱导大鼠急性肾损伤模型的血清肌酐和乳酸浓度，减轻肾小管坏死和炎症损伤。Landiolol 可能不通过全身抗炎或抗氧化作用介导肾脏保护作用[2]。
Landiolol 对心脏功能的影响小于 Esmolol (HY-B1392A)，不会直接缩短动作电位时程 (APD)[3]。

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

Animal Model: LPS-induced Acute Kidney Injury Rat Model (250-300 g，6-8 weeks old)[2]
Dosage: 0.1 mg/kg/min
Administration: Continuous intravenous infusion starting at the time of LPS administration (7.5 mg/kg, iv), maintained for 6 h
Result: Significantly improved renal function compared to the LPS group.
Decreased serum creatinine levels to 0.7 ± 0.3 mg/mL versus 1.4 ± 0.7 mg/mL in the LPS group, and decreased lactate levels to 3.8 ± 0.7 mmol/L versus 6.5 ± 1.3 mmol/L, at 6 h.
Reduced tubular degeneration, dilation, and acute necrosis in the renal cortex and medulla in the landiolol group compared to the LPS group.
Urinary 8-OHdG, a marker of oxidative stress, was increased in both groups but not significantly different between them, indicating landiolol’s renoprotection was not mediated by systemic anti-inflammatory or antioxidant effects.
Clinical Trial
分子量

509.59

Formula

C25H39N3O8
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

Landiolol 相关分类

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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:

Landiolol133242-30-5ONO1101ONO 1101ONO-1101Adrenergic ReceptorCalcium ChannelPotassium ChannelReactive Oxygen Species (ROS)Beta ReceptorCa2+ channelsCa channelsKcsAInhibitorinhibitorinhibit

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