Landiolol HCl
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MedKoo CAT#: 326680

CAS#: 144481-98-1 (HCl)

Description: Landiolol, also known as LDLL600 and ONO 1101, is an ultra-short-acting β1-blocker, is useful for managing supraventricular tachyarrhythmias in sepsis. Landiolol is a drug which acts as a highly cardioselective, ultra short-acting beta blocker. It is used as an anti-arrhythmic agent. Landiolol reduces hemodynamic responses to bronchoscopy-assisted suctioning in intubated ICU patients.

Chemical Structure

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Landiolol HCl
CAS# 144481-98-1 (HCl)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 326680
Name: Landiolol HCl
CAS#: 144481-98-1 (HCl)
Chemical Formula: C25H40ClN3O8
Exact Mass: 545.25
Molecular Weight: 546.058
Elemental Analysis: C, 54.99; H, 7.38; Cl, 6.49; N, 7.70; O, 23.44

Price and Availability

Size Price Availability Quantity
50mg USD 350 2 Weeks
250mg USD 950 2 Weeks
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Related CAS #: 144481-98-1 (HCl)   133242-30-5 (free base)    

Synonym: LDLL600; LDLL 600; LDLL-600; ONO1101; ONO-1101; ONO 1101 hydrochloride; Landiolol; Landiolol HCl; Landiolol hydrochloride.

IUPAC/Chemical Name: (2,2-dimethyl-1,3-dioxolan-4-yl)methyl 3-(4-((S)-2-hydroxy-3-((2-(morpholine-4-carboxamido)ethyl)amino)propoxy)phenyl)propanoate hydrochloride

InChi Key: DLPGJHSONYLBKP-CNAJMHLNSA-N

InChi Code: InChI=1S/C25H39N3O8.ClH/c1-25(2)35-18-22(36-25)17-34-23(30)8-5-19-3-6-21(7-4-19)33-16-20(29)15-26-9-10-27-24(31)28-11-13-32-14-12-28;/h3-4,6-7,20,22,26,29H,5,8-18H2,1-2H3,(H,27,31);1H/t20-,22?;/m0./s1

SMILES Code: O=C(OCC1OC(C)(C)OC1)CCC2=CC=C(OC[C@@H](O)CNCCNC(N3CCOCC3)=O)C=C2.[H]Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
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Biological target: Landiolol hydrochloride (ONO1101 hydrochloride) is a highly beta1 selective ultra-short acting beta-blocker (β1/β2 selectivity = 255:1, a half-life of 4 min), acts as an adrenoceptor antagonist.
In vitro activity: TBD
In vivo activity: ONO-1101 significantly decreased the heart rate, rate-pressure product, left ventricular contraction, cardiac output, and relative refractory period of the right ventricle, suppressed the AV nodal conduction, and increased the effective refractory period of the right ventricle, whereas no significant change was observed in the preload and afterload of the left ventricle, intrinsic sinus nodal automaticity, His-Purkinje-ventricular conduction, and the monophasic action-potential duration of the right ventricle in beagle dogs. These results suggest that the suppressive effects of ONO-1101 on cardiovascular performance are significantly less potent than those of esmolol at equipotent beta-blocking doses. Reference: J Cardiovasc Pharmacol. 1999 Jul;34(1):70-7. https://pubmed.ncbi.nlm.nih.gov/10413070/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 175.0 320.48
Ethanol 42.0 76.91
Water 100.0 183.13

Preparing Stock Solutions

The following data is based on the product molecular weight 546.06 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Sugiyama A, Takahara A, Hashimoto K. Electrophysiologic, cardiohemodynamic and beta-blocking actions of a new ultra-short-acting beta-blocker, ONO-1101, assessed by the in vivo canine model in comparison with esmolol. J Cardiovasc Pharmacol. 1999 Jul;34(1):70-7. doi: 10.1097/00005344-199907000-00012. PMID: 10413070. 2. Ahmet I, Fukushima N, Sawa Y, Masai T, Kadoba K, Kagisaki K, Chang JC, Yamaguchi T, Matsuda H. The effects of a new ultra-short-acting beta-adrenergic blocker, ONO-1101, on cardiac function during and after cardiopulmonary bypass. Surg Today. 1999;29(3):248-54. doi: 10.1007/BF02483015. PMID: 10192736.
In vitro protocol: TBD
In vivo protocol: 1. Sugiyama A, Takahara A, Hashimoto K. Electrophysiologic, cardiohemodynamic and beta-blocking actions of a new ultra-short-acting beta-blocker, ONO-1101, assessed by the in vivo canine model in comparison with esmolol. J Cardiovasc Pharmacol. 1999 Jul;34(1):70-7. doi: 10.1097/00005344-199907000-00012. PMID: 10413070. 2. Ahmet I, Fukushima N, Sawa Y, Masai T, Kadoba K, Kagisaki K, Chang JC, Yamaguchi T, Matsuda H. The effects of a new ultra-short-acting beta-adrenergic blocker, ONO-1101, on cardiac function during and after cardiopulmonary bypass. Surg Today. 1999;29(3):248-54. doi: 10.1007/BF02483015. PMID: 10192736.

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1: Wada Y, Aiba T, Tsujita Y, Itoh H, Wada M, Nakajima I, Ishibashi K, Okamura H, Miyamoto K, Noda T, Sugano Y, Kanzaki H, Anzai T, Kusano K, Yasuda S, Horie M, Ogawa H. Practical applicability of landiolol, an ultra-short-acting β1-selective blocker, for rapid atrial and ventricular tachyarrhythmias with left ventricular dysfunction. J Arrhythm. 2016 Apr;32(2):82-8. doi: 10.1016/j.joa.2015.09.002. Epub 2015 Nov 2. PubMed PMID: 27092187; PubMed Central PMCID: PMC4823575.

2: Takata J, Haruyama N, Arashi T, Mae T. Alteration of fatal 1:1 conducted atrial flutter to less conducted ratio by landiolol infusion. J Anesth. 2016 Apr 16. [Epub ahead of print] PubMed PMID: 27085543.

3: Kido T, Mochizuki T, Hirano M, Yamada Y, Tanaka R, Kanzaki S, Higashi M, Jinzaki M, Yoshioka K, Kuribayashi S. Radiation-Dose-Lowering Effects of Landiolol Hydrochloride in Coronary Angiography Using Computed Tomography (DELIGHT)　- A Prospective Multicenter Study. Circ J. 2016 Apr 25;80(5):1225-31. doi: 10.1253/circj.CJ-15-0962. Epub 2016 Mar 28. PubMed PMID: 27019983.

4: Tachi K, Takahashi S, Tanaka M. [Relationship between the Landiolol Dose and Urinary Catecholamine Metabolites in the Perioperative Management of Patients Undergoing Pheochromocytoma Resection]. Masui. 2015 Dec;64(12):1234-8. Japanese. PubMed PMID: 26790322.

5: Shibata SC, Uchiyama A, Ohta N, Fujino Y. Efficacy and Safety of Landiolol Compared to Amiodarone for the Management of Postoperative Atrial Fibrillation in Intensive Care Patients. J Cardiothorac Vasc Anesth. 2016 Apr;30(2):418-22. doi: 10.1053/j.jvca.2015.09.007. Epub 2015 Sep 25. PubMed PMID: 26703973.

6: Miyake K, Fujita Y, Yoshizawa S, Tomita M, Miyazu M, Sento Y, Yoshimura S, Sobue K. Effects of landiolol on refractory tachyarrhythmia after total cavopulmonary connection: a retrospective, observational, cohort study. J Anesth. 2016 Apr;30(2):331-6. doi: 10.1007/s00540-015-2119-4. Epub 2015 Dec 23. PubMed PMID: 26699148.

7: Ishigaki D, Arimoto T, Iwayama T, Hashimoto N, Kutsuzawa D, Kumagai Y, Nishiyama S, Takahashi H, Shishido T, Miyamoto T, Watanabe T, Kubota I. Prevention of immediate recurrence of atrial fibrillation with low-dose landiolol after radiofrequency catheter ablation. J Arrhythm. 2015 Oct;31(5):279-85. doi: 10.1016/j.joa.2015.02.003. Epub 2015 Apr 4. PubMed PMID: 26550083; PubMed Central PMCID: PMC4600890.

8: Li L, Ai Q, Lin L, Ge P, Yang C, Zhang L. Efficacy and safety of landiolol for prevention of atrial fibrillation after cardiac surgery: a meta-analysis of randomized controlled trials. Int J Clin Exp Med. 2015 Jul 15;8(7):10265-73. eCollection 2015. Review. PubMed PMID: 26379818; PubMed Central PMCID: PMC4565201.

9: Nitta D, Kinugawa K, Imamura T, Endo M, Amiya E, Inaba T, Maki H, Hatano M, Komuro I. An Experience of Landiolol Use for an Advanced Heart Failure Patient With Severe Hypotension. Int Heart J. 2015;56(5):564-7. doi: 10.1536/ihj.15-103. Epub 2015 Sep 11. PubMed PMID: 26370372.

10: Kanamori K, Aoyagi T, Mikamo T, Tsutsui K, Kunishima T, Inaba H, Hayami N, Murakawa Y. Successful Treatment of Refractory Electrical Storm With Landiolol After More Than 100 Electrical Defibrillations. Int Heart J. 2015;56(5):555-7. doi: 10.1536/ihj.15-102. Epub 2015 Sep 4. PubMed PMID: 26346519.

11: Okajima M, Takamura M, Taniguchi T. 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. doi: 10.5492/wjccm.v4.i3.251. eCollection 2015 Aug 4. PubMed PMID: 26261777; PubMed Central PMCID: PMC4524822.

12: Sezai A, Osaka S, Yaoita H, Ishii Y, Arimoto M, Hata H, Shiono M. Safety and efficacy of landiolol hydrochloride for prevention of atrial fibrillation after cardiac surgery in patients with left ventricular dysfunction: Prevention of Atrial Fibrillation After Cardiac Surgery With Landiolol Hydrochloride for Left Ventricular Dysfunction (PLATON) trial. J Thorac Cardiovasc Surg. 2015 Oct;150(4):957-64. doi: 10.1016/j.jtcvs.2015.07.003. Epub 2015 Jul 10. PubMed PMID: 26254752.

13: Yamashita Y, Iguchi M, Nakatani R, Usui T, Takagi D, Hamatani Y, Unoki T, Ishii M, Ogawa H, Masunaga N, Abe M, Akao M. Thyroid Storm with Heart Failure Treated with a Short-acting Beta-adrenoreceptor Blocker, Landiolol Hydrochloride. Intern Med. 2015;54(13):1633-7. doi: 10.2169/internalmedicine.54.3138. Epub 2015 Jul 1. PubMed PMID: 26134196.

14: Deguchi S, Komasawa N, Fujiwara S, Kido H, Minami T. [Successful sedation with landiolol and dexmedetomidine during spinal anesthesia in a patient with active dementia]. Masui. 2015 Jan;64(1):95-7. Japanese. PubMed PMID: 25868211.

15: Oka H, Sugimoto M, Azuma H. Efficacy of landiolol for the treatment of junctional ectopic tachycardia resulting from sepsis. Cardiol Young. 2016 Jan;26(1):183-7. doi: 10.1017/S1047951115000244. Epub 2015 Mar 18. PubMed PMID: 25785611.

16: Kunisawa T, Yamagishi A, Suno M, Nakade S, Honda N, Kurosawa A, Sugawara A, Tasaki Y, Iwasaki H. Target-controlled infusion and population pharmacokinetics of landiolol hydrochloride in patients with peripheral arterial disease. Ther Clin Risk Manag. 2015 Jan 17;11:107-14. doi: 10.2147/TCRM.S74867. eCollection 2015. PubMed PMID: 25653534; PubMed Central PMCID: PMC4303402.

17: Hifumi T, Kato H, Koido Y, Kawakita K, Kuroda Y. Safety and effective use of landiolol in the ICU. J Intensive Care. 2014 Feb 21;2(1):16. doi: 10.1186/2052-0492-2-16. eCollection 2014. PubMed PMID: 25520832; PubMed Central PMCID: PMC4267602.

18: Tochikubo J, Adachi YU, Ejima T, Numaguchi A, Matsuda N, Sato S, Shiiya N. Landiolol reduces hemodynamic responses to bronchoscopy-assisted suctioning in intubated ICU patients. J Intensive Care. 2014 Jan 23;2(1):6. doi: 10.1186/2052-0492-2-6. eCollection 2014. PubMed PMID: 25520823; PubMed Central PMCID: PMC4267460.

19: Yamashita T, Saitoh T, Matsushita M. Design of a prospective observational survey on landiolol in atrial fibrillation/atrial flutter patients with chronic heart failure - AF-CHF landiolol survey. J Cardiol. 2015 Jul;66(1):69-72. doi: 10.1016/j.jjcc.2014.09.008. Epub 2014 Nov 6. PubMed PMID: 25454208.

20: Niwa Y, Koike M, Iwata N, Kobayashi D, Tanaka C, Fujii T, Nakayama G, Sugimoto H, Fujiwara M, Kodera Y. Effect of landiolol hydrochloride on tachyarrhythmia after esophagectomy. Hepatogastroenterology. 2014 Sep;61(134):1546-51. PubMed PMID: 25436340.