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MedKoo Cat#: 584392 | Name: Esmolol
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Esmolol is a short acting hyperselective β-adrenergic blocker effective in blunting adrenergic response to several perioperative stimuli and so it might interfere in the effect of the anesthetic drugs on the brain. Esmolol is effective not only in attenuating intraoperative hemodynamic changes related to sympathetic overdrive but also in minimizing significant propofol and sevoflurane requirements without compromising the hemodynamic status.

Chemical Structure

Esmolol
Esmolol
CAS#81147-92-4 (free base)

Theoretical Analysis

MedKoo Cat#: 584392

Name: Esmolol

CAS#: 81147-92-4 (free base)

Chemical Formula: C16H25NO4

Exact Mass: 295.1784

Molecular Weight: 295.38

Elemental Analysis: C, 65.06; H, 8.53; N, 4.74; O, 21.67

Price and Availability

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100mg USD 850.00 2 weeks
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Related CAS #
81147-92-4 (free base) 81161-17-3 (HCl)
Synonym
Esmolol; (+-)-Esmolol; (+/-)-esmolol; Esmololum; ASL-8052-001; ASL 8052-001;
IUPAC/Chemical Name
Benzenepropanoic acid, 4-(2-hydroxy-3-((1-methylethyl)amino)propoxy)-, methyl ester
InChi Key
AQNDDEOPVVGCPG-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H25NO4/c1-12(2)17-10-14(18)11-21-15-7-4-13(5-8-15)6-9-16(19)20-3/h4-5,7-8,12,14,17-18H,6,9-11H2,1-3H3
SMILES Code
O=C(OC)CCC1=CC=C(OCC(O)CNC(C)C)C=C1
Appearance
Solid powder
Purity
>95% (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
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
View handling instruction
Biological target:
Esmolol is a cardioselective beta1 receptor blocker.
In vitro activity:
The results indicated that esmolol reversibly inhibited I(Na) in a concentration-dependent manner, with an IC50 of 74.2 +/- 0.60 micromol l(-1) with a Hill coefficient of 1.02 +/- 0.04. This inhibition was voltage- and frequency-dependent. Reference: Methods Find Exp Clin Pharmacol. 2006 Dec;28(10):697-702. https://pubmed.ncbi.nlm.nih.gov/17235414/
In vivo activity:
Brain histology showed a significant reduction in cortical neuronal degeneration/necrosis in the esmolol group compared to the control one (mean score 0.3 vs. 1.3, p = 0.03, Fig. 3A), while only a trend was present in the hippocampal region (mean score 1 vs. 2, p = 0.11, Fig. 3B). A marked reduction of microglial activation in the hippocampus was also observed after treatment with esmolol compared to control (mean % 6 vs. 2, p < 0.001, Fig. 3C). Significantly lower circulating levels of NSE were measured in esmolol animals compared to controls at 96 h after resuscitation (median 2.2 vs. 21, p < 0.0001, Fig. 4A). Reference: Sci Rep. 2021; 11: 10635. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8138021/
Solvent mg/mL mM
Solubility
DMSO 59.0 199.74
Ethanol 59.0 199.74
Water 59.0 199.74
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 295.38 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. Deng CY, Lin SG, Zhang WC, Kuang SJ, Qian WM, Wu SL, Shan ZX, Yang M, Yu XY. Esmolol inhibits Na+ current in rat ventricular myocytes. Methods Find Exp Clin Pharmacol. 2006 Dec;28(10):697-702. doi: 10.1358/mf.2006.28.10.1037498. PMID: 17235414. 2. Gorelik J, Vodyanoy I, Shevchuk AI, Diakonov IA, Lab MJ, Korchev YE. Esmolol is antiarrhythmic in doxorubicin-induced arrhythmia in cultured cardiomyocytes - determination by novel rapid cardiomyocyte assay. FEBS Lett. 2003 Jul 31;548(1-3):74-8. doi: 10.1016/s0014-5793(03)00743-9. PMID: 12885410. 3. Ruggeri L, Nespoli F, Ristagno G, Fumagalli F, Boccardo A, Olivari D, Affatato R, Novelli D, De Giorgio D, Romanelli P, Minoli L, Cucino A, Babini G, Staszewsky L, Zani D, Pravettoni D, Belloli A, Scanziani E, Latini R, Magliocca A. Esmolol during cardiopulmonary resuscitation reduces neurological injury in a porcine model of cardiac arrest. Sci Rep. 2021 May 20;11(1):10635. doi: 10.1038/s41598-021-90202-w. PMID: 34017043; PMCID: PMC8138021. 4. Hoareau GL, Beyer CA, Caples CM, Spruce MW, Gilbert Z, Grayson JK, Neff LP, Williams TK, Johnson MA. Esmolol reduces myocardial injury induced by resuscitative endovascular balloon occlusion of the aorta (REBOA) in a porcine model of hemorrhagic shock. Injury. 2020 Oct;51(10):2165-2171. doi: 10.1016/j.injury.2020.07.005. Epub 2020 Jul 3. PMID: 32669205.
In vitro protocol:
1. Deng CY, Lin SG, Zhang WC, Kuang SJ, Qian WM, Wu SL, Shan ZX, Yang M, Yu XY. Esmolol inhibits Na+ current in rat ventricular myocytes. Methods Find Exp Clin Pharmacol. 2006 Dec;28(10):697-702. doi: 10.1358/mf.2006.28.10.1037498. PMID: 17235414. 2. Gorelik J, Vodyanoy I, Shevchuk AI, Diakonov IA, Lab MJ, Korchev YE. Esmolol is antiarrhythmic in doxorubicin-induced arrhythmia in cultured cardiomyocytes - determination by novel rapid cardiomyocyte assay. FEBS Lett. 2003 Jul 31;548(1-3):74-8. doi: 10.1016/s0014-5793(03)00743-9. PMID: 12885410.
In vivo protocol:
1. Ruggeri L, Nespoli F, Ristagno G, Fumagalli F, Boccardo A, Olivari D, Affatato R, Novelli D, De Giorgio D, Romanelli P, Minoli L, Cucino A, Babini G, Staszewsky L, Zani D, Pravettoni D, Belloli A, Scanziani E, Latini R, Magliocca A. Esmolol during cardiopulmonary resuscitation reduces neurological injury in a porcine model of cardiac arrest. Sci Rep. 2021 May 20;11(1):10635. doi: 10.1038/s41598-021-90202-w. PMID: 34017043; PMCID: PMC8138021. 2. Hoareau GL, Beyer CA, Caples CM, Spruce MW, Gilbert Z, Grayson JK, Neff LP, Williams TK, Johnson MA. Esmolol reduces myocardial injury induced by resuscitative endovascular balloon occlusion of the aorta (REBOA) in a porcine model of hemorrhagic shock. Injury. 2020 Oct;51(10):2165-2171. doi: 10.1016/j.injury.2020.07.005. Epub 2020 Jul 3. PMID: 32669205.
1: Dimopoulos G, Theodorakopoulou M, Armaganidis A, Tzepi IM, Lignos M, Giamarellos-Bourboulis EJ, Tsaganos T. Esmolol: immunomodulator in pyelonephritis by Pseudomonas aeruginosa. J Surg Res. 2015 Sep;198(1):175-84. doi: 10.1016/j.jss.2015.05.026. Epub 2015 May 21. PubMed PMID: 26073350. 2: Morelli A, Ertmer C, Westphal M, Rehberg S, Kampmeier T, Ligges S, Orecchioni A, D'Egidio A, D'Ippoliti F, Raffone C, Venditti M, Guarracino F, Girardis M, Tritapepe L, Pietropaoli P, Mebazaa A, Singer M. Effect of heart rate control with esmolol on hemodynamic and clinical outcomes in patients with septic shock: a randomized clinical trial. JAMA. 2013 Oct 23;310(16):1683-91. doi: 10.1001/jama.2013.278477. PubMed PMID: 24108526. 3: Ono H, Ohtani N, Matoba A, Kido K, Yasui Y, Masaki E. Efficacy of intrathecal esmolol on heat-evoked responses in a postoperative pain model. Am J Ther. 2015 Mar-Apr;22(2):111-6. doi: 10.1097/MJT.0b013e318274e0a1. PubMed PMID: 23411610. 4: Asouhidou I, Trikoupi A. Esmolol reduces anesthetic requirements thereby facilitating early extubation; a prospective controlled study in patients undergoing intracranial surgery. BMC Anesthesiol. 2015 Nov 28;15:172. doi: 10.1186/s12871-015-0154-1. PubMed PMID: 26615516; PubMed Central PMCID: PMC4663038. 5: Tao Y, Jingyi W, Xiaogan J, Weihua L, Xiaoju J. [Effect of esmolol on fluid responsiveness and hemodynamic parameters in patients with septic shock]. Zhonghua Wei Zhong Bing Ji Jiu Yi Xue. 2015 Nov;27(11):885-9. Chinese. PubMed PMID: 27132454. 6: Dahle GO, Salminen PR, Moen CA, Eliassen F, Jonassen AK, Haaverstad R, Matre K, Grong K. Esmolol added in repeated, cold, oxygenated blood cardioplegia improves myocardial function after cardiopulmonary bypass. J Cardiothorac Vasc Anesth. 2015;29(3):684-93. doi: 10.1053/j.jvca.2014.09.017. Epub 2015 Jan 6. PubMed PMID: 25575405. 7: Driver BE, Debaty G, Plummer DW, Smith SW. Use of esmolol after failure of standard cardiopulmonary resuscitation to treat patients with refractory ventricular fibrillation. Resuscitation. 2014 Oct;85(10):1337-41. doi: 10.1016/j.resuscitation.2014.06.032. Epub 2014 Jul 14. PubMed PMID: 25033747. 8: Wang Z, Wu Q, Nie X, Guo J, Yang C. Combination therapy with milrinone and esmolol for heart protection in patients with severe sepsis: a prospective, randomized trial. Clin Drug Investig. 2015 Nov;35(11):707-16. doi: 10.1007/s40261-015-0325-3. PubMed PMID: 26387030. 9: Maurovich-Horvat P, Károlyi M, Horváth T, Szilveszter B, Bartykowszki A, Jermendy ÁL, Panajotu A, Celeng C, Suhai FI, Major GP, Csobay-Novák C, Hüttl K, Merkely B. Esmolol is noninferior to metoprolol in achieving a target heart rate of 65 beats/min in patients referred to coronary CT angiography: a randomized controlled clinical trial. J Cardiovasc Comput Tomogr. 2015 Mar-Apr;9(2):139-45. doi: 10.1016/j.jcct.2015.02.001. Epub 2015 Feb 14. PubMed PMID: 25819196. 10: Xinqiang L, Weiping H, Miaoyun W, Wenxin Z, Wenqiang J, Shenglong C, Juhao Z, Hongki Z. [Esmolol improves clinical outcome and tissue oxygen metabolism in patients with septic shock through controlling heart rate]. Zhonghua Wei Zhong Bing Ji Jiu Yi Xue. 2015 Sep;27(9):759-63. Chinese. PubMed PMID: 26955704. 11: Zhang L, Nie Y, Zheng Y, Ke L, Tong Z, Li W, Li J. Esmolol attenuates lung injury and inflammation in severe acute pancreatitis rats. Pancreatology. 2016 Sep-Oct;16(5):726-32. doi: 10.1016/j.pan.2016.05.395. Epub 2016 May 30. PubMed PMID: 27269252. 12: Harless M, Depp C, Collins S, Hewer I. Role of Esmolol in Perioperative Analgesia and Anesthesia: A Literature Review. AANA J. 2015 Jun;83(3):167-77. Review. PubMed PMID: 26137757. 13: McKee JS, Rabinow BE, Daller JR, Brooks BD, Baumgartner B, Rohatgi P. An enantiomerically pure formulation of esmolol attenuates hypotension and preserves heart rate control in dogs. Anesthesiology. 2014 Dec;121(6):1184-93. doi: 10.1097/ALN.0000000000000408. PubMed PMID: 25105423. 14: Wang Z, Wu Q, Nie X, Guo J, Yang C. Infusion of esmolol attenuates lipopolysaccharide-induced myocardial dysfunction. J Surg Res. 2016 Jan;200(1):283-9. doi: 10.1016/j.jss.2015.07.015. Epub 2015 Jul 14. PubMed PMID: 26316443. 15: Zoerner F, Lennmyr F, Wiklund L, Martijn C, Semenas E. Milrinone and esmolol decrease cardiac damage after resuscitation from prolonged cardiac arrest. Acta Anaesthesiol Scand. 2015 Apr;59(4):465-74. doi: 10.1111/aas.12480. Epub 2015 Feb 27. PubMed PMID: 25790148. 16: Bebawy JF, Houston CC, Kosky JL, Badri AM, Hemmer LB, Moreland NC, Carabini LM, Koht A, Gupta DK. Nicardipine is superior to esmolol for the management of postcraniotomy emergence hypertension: a randomized open-label study. Anesth Analg. 2015 Jan;120(1):186-92. doi: 10.1213/ANE.0000000000000473. PubMed PMID: 25296247. 17: Aguiar Rosa S, Ramos R, Marques H, Santos R, Leal C, Casado H, Saraiva M, Figueiredo L, Cruz Ferreira R. Bailout intravenous esmolol for heart rate control in cardiac computed tomography angiography. Rev Port Cardiol. 2016 Dec;35(12):673-678. doi: 10.1016/j.repc.2016.07.004. Epub 2016 Nov 17. English, Portuguese. PubMed PMID: 27865676. 18: Du W, Wang XT, Long Y, Liu DW. Efficacy and Safety of Esmolol in Treatment of Patients with Septic Shock. Chin Med J (Engl). 2016 Jul 20;129(14):1658-65. doi: 10.4103/0366-6999.185856. PubMed PMID: 27411452; PubMed Central PMCID: PMC4960954. 19: Ergil J, Kavak Akelma F, Özkan D, Bumin Aydin G, Gürel A, Akinci M. Effects of pretreatment with esmolol and lidocaine on injection pain and rocuronium-induced withdrawal response. Turk J Med Sci. 2015;45(4):959-63. PubMed PMID: 26422874. 20: Shang X, Wang K, Xu J, Gong S, Ye Y, Chen K, Lian F, Chen W, Yu R. The Effect of Esmolol on Tissue Perfusion and Clinical Prognosis of Patients with Severe Sepsis: A Prospective Cohort Study. Biomed Res Int. 2016;2016:1038034. doi: 10.1155/2016/1038034. Epub 2016 Aug 29. PubMed PMID: 27652257; PubMed Central PMCID: PMC5019858.