Landiolol
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 133242-30-5
- 分子式: C25H39N3O8
- 分子量:509.59
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
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Beta-1 adrenergic receptor |
L-type calcium channel |
IrK |
体外実験
Landiolol (10 μM; 24 h) significantly inhibits the increase in mitochondrial oxygen consumption rate (OCR) induced by TNF-α (0.5 nM) in HEK293 cells, reducing the basal OCR from 123% to 94.8%, and reduces the generation of reactive oxygen species (ROS)[1].
Landiolol (10 μM; 24 h) inhibits the excessive glycolytic capacity of HEK293 cells induced by TNF-α (0.5 nM), but does not significantly affect its basal glycolytic (ECAR) level[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HEK293 cells
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Concentration:10 μM (Landiolol)
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Incubation Time:24 h; with 0.5 nM TNF-α
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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.
体内実験
Landiolol has less effect on cardiac function than Esmolol (HY-B1392A) and does not directly shorten the action potential duration (APD)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS-induced Acute Kidney Injury Rat Model (250-300 g，6-8 weeks old)[2]
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Dosage:0.1 mg/kg/min
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Administration:Continuous intravenous infusion starting at the time of LPS administration (7.5 mg/kg, iv), maintained for 6 h
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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.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 133242-30-5
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分子量 509.59
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分子式 C25H39N3O8
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SMILES
O=C(OC[C@H]1OC(C)(C)OC1)CCC2=CC=C(OC[C@@H](O)CNCCNC(N3CCOCC3)=O)C=C2
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別名
ONO1101
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Nephrotoxicity Study
This protocol assesses nephrotoxicity by combining functional kidney injury readouts, urinary/tissue injury biomarkers, and renal histopathology. Serum creatinine and BUN reflect impaired kidney function, while KIM-1, NGAL, clusterin, osteopontin, IL-18, cystatin C, nephrin, Oat5, urinary protein, glucose, and alkaline phosphatase have been used to detect tubular injury in cisplatin-, gentamicin-, and acetaminophen-induced nephrotoxicity models.
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LPS-Induced Endotoxemia/Systemic Inflammation
Lipopolysaccharide (LPS)-induced endotoxemia is a widely used in vivo model of acute systemic inflammation in which LPS, a Gram-negative bacterial endotoxin, activates innate immune signaling primarily through TLR4, leading to rapid and transient induction of pro-inflammatory cytokines such as TNF-α, IL-6, and IL-1β in circulation and tissues. This cytokine surge is commonly used as a measurable readout of systemic inflammatory activation and immune dysregulation, and is typically assessed within hours after intraperitoneal LPS administration in mouse models of endotoxemia. The model captures key features of systemic inflammatory response syndrome, including cytokine release, immune cell activation, and downstream tissue responses, and has been used to evaluate anti-inflammatory interventions such as cytokine modulation, lipid mediators, and immune cell-targeting therapies.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
純度とドキュメンテーション
参考文献
[1]. Tomihari M, et al. Propranolol and landiolol inhibit cell proliferation enhanced by noradrenaline in human lung adenocarcinoma cells. Biomed Res. 2024;45(6):253-259. [Content Brief]
[2]. Kiyonaga N, et al. Effects of Landiolol in Lipopolysaccharide-Induced Acute Kidney Injury in Rats and In Vitro. Shock. 2019 Nov;52(5):e117-e123. [Content Brief]
[3]. Shibata S, et al. Direct effects of esmolol and landiolol on cardiac function, coronary vasoactivity, and ventricular electrophysiology in guinea-pig hearts. J Pharmacol Sci. 2012;118(2):255-65. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Landiolol 関連分類
HY-100607 関連分類
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