Landiolol hydrochloride (Synonyms: ONO1101 hydrochloride)

Name: Landiolol hydrochloride
Brand: MedChemExpress
SKU: HY-100607A
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Cat. No.: HY-100607A Pureza: 99.82%: Ficha de datos
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Landiolol (ONO1101) hydrochloride is a highly selective, ultra-short-acting competitive inhibitor of β₁ adrenergic receptors. Landiolol hydrochloride specifically blocks cardiac β₁ receptors, reducing heart rate and myocardial oxygen consumption. Landiolol hydrochloride inhibits TNF-α-induced excessive mitochondrial oxygen consumption and reactive oxygen species production in a sepsis model, alleviating renal injury. Landiolol hydrochloride 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 hydrochloride can be used for perioperative tachycardia control and protection studies of sepsis-related acute kidney injury.

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Landiolol hydrochloride Estructura química

No. CAS : 144481-98-1

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtener un presupuesto
500 mg	Obtener un presupuesto

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Other Forms of Landiolol hydrochloride:

Landiolol Obtener un presupuesto
Landiolol hydrochloride (Standard) Obtener un presupuesto

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Adrenergic Receptor:

Ver todas las isoformas

α adrenergic receptor β adrenergic receptor

Ver todos los productos específicos de isoformas Calcium Channel:

Ver todas las isoformas

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

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Referencias
Revisión del cliente

Descripciòn

IC₅₀ & Target

Beta-1 adrenergic receptor

L-type calcium channel

IrK

In Vitro

Landiolol hydrochloride (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 hydrochloride (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.

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.

In Vivo

Landiolol (0.1 mg/kg/min; intravenous infusion; single dose; 6 h) hydrochloride significantly reduces serum creatinine and lactate concentrations and alleviates renal tubular necrosis and inflammatory damage in the lipopolysaccharide (LPS)-induced acute kidney injury model in rats. Landiolol hydrochloride may not mediate renal protection through systemic anti-inflammatory or antioxidant effects^[2].
Landiolol hydrochloride 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.

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.

Peso molecular

546.05

Fòrmula

C₂₅H₄₀ClN₃O₈

No. CAS

144481-98-1

Appearance

Solid

Color

White to off-white

SMILES

O=C(OC[C@H]1OC(C)(C)OC1)CCC2=CC=C(OC[C@@H](O)CNCCNC(N3CCOCC3)=O)C=C2.[H]Cl

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

4°C, sealed storage, away from moisture

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

Solvente y solubilidad

In Vitro:

DMSO : 250 mg/mL (457.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 100 mg/mL (183.13 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8313 mL	9.1567 mL	18.3133 mL
5 mM	0.3663 mL	1.8313 mL	3.6627 mL
10 mM	0.1831 mL	0.9157 mL	1.8313 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Calculadora de molaridad
Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Pureza y Documentación

Purity: 99.96%

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Ficha de datos (275 KB) SDS (393 KB)

COA (244 KB) LCMS (109 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Atarashi H, et al. Pharmacokinetics of landiolol hydrochloride, a new ultra-short-acting beta-blocker, in patients with cardiac arrhythmias. Clin Pharmacol Ther. 2000 Aug;68(2):143-50. [Content Brief]

[2]. Okajima M, et al. Landiolol, an ultra-short-acting β1-blocker, is useful for managing supraventricular tachyarrhythmias in sepsis. World J Crit Care Med. 2015 Aug 4;4(3):251-7. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.8313 mL	9.1567 mL	18.3133 mL	45.7834 mL
	5 mM	0.3663 mL	1.8313 mL	3.6627 mL	9.1567 mL
	10 mM	0.1831 mL	0.9157 mL	1.8313 mL	4.5783 mL
	15 mM	0.1221 mL	0.6104 mL	1.2209 mL	3.0522 mL
	20 mM	0.0916 mL	0.4578 mL	0.9157 mL	2.2892 mL
	25 mM	0.0733 mL	0.3663 mL	0.7325 mL	1.8313 mL
	30 mM	0.0610 mL	0.3052 mL	0.6104 mL	1.5261 mL
	40 mM	0.0458 mL	0.2289 mL	0.4578 mL	1.1446 mL
	50 mM	0.0366 mL	0.1831 mL	0.3663 mL	0.9157 mL
	60 mM	0.0305 mL	0.1526 mL	0.3052 mL	0.7631 mL
	80 mM	0.0229 mL	0.1145 mL	0.2289 mL	0.5723 mL
	100 mM	0.0183 mL	0.0916 mL	0.1831 mL	0.4578 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Landiolol hydrochloride Related Classifications

Inflammation/Immunology Endocrinology Cardiovascular Disease

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:

Landiolol144481-98-1ONO1101ONO 1101ONO-1101Adrenergic ReceptorCalcium ChannelPotassium ChannelReactive Oxygen Species (ROS)Beta ReceptorCa2+ channelsCa channelsKcsAInhibitorinhibitorinhibit

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Landiolol hydrochloride (Synonyms: ONO1101 hydrochloride)

Revisión del cliente

Other Forms of Landiolol hydrochloride:

Landiolol hydrochloride Related Antibodies

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Adrenergic Receptor:

Ver todos los productos específicos de isoformas Calcium Channel:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Landiolol hydrochloride Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Landiolol hydrochloride Related Classifications

Keywords:

Productos vistos recientemente:

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