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.
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- CAS No.: 133242-30-5
- 화학식: C25H39N3O8
- 분자량:509.59
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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Beta-1 adrenergic receptor |
L-type calcium channel |
IrK |
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.
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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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 133242-30-5
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분자량 509.59
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화학식 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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Synonyms
ONO1101
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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