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MedKoo Cat#: 562874 | Name: Dexmedetomidine HCl
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Description:

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

Dexmedetomidine is a potent α-2-adrenergic agonist. Dexmedetomidine is an anxiolytic, sedative, and analgesic agent. Similar to clonidine, it is an agonist of α2-adrenergic receptors in certain parts of the brain. Dexmedetomidine is notable for its ability to provide sedation without risk of respiratory depression (unlike other commonly used sedatives such as propofol, fentanyl, and midazolam) and can provide cooperative or semi-arousable sedation. Dexmedetomidine is also used in veterinary agent for dogs and cats.

Chemical Structure

Dexmedetomidine HCl
Dexmedetomidine HCl
CAS#145108-58-3 (HCl)

Theoretical Analysis

MedKoo Cat#: 562874

Name: Dexmedetomidine HCl

CAS#: 145108-58-3 (HCl)

Chemical Formula: C13H17ClN2

Exact Mass: 0.0000

Molecular Weight: 236.74

Elemental Analysis: C, 65.95; H, 7.24; Cl, 14.97; N, 11.83

Price and Availability

Size Price Availability Quantity
100mg USD 450.00 2 Weeks
1g USD 2,450.00 2 Weeks
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Related CAS #
145108-58-3 (HCl) 113775-47-6 (free base)
Synonym
Dexmedetomidine HCl; Dexmedetomidine Hydrochloride; Precedex; Dexdomitor; (+)-Medetomidine Hydrochloride; BXCL-501; BXCL 501; BXCL501;
IUPAC/Chemical Name
5-[(1S)-1-(2,3-Dimethylphenyl)ethyl]-1H-imidazole;hydrochloride
InChi Key
VPNGEIHDPSLNMU-MERQFXBCSA-N
InChi Code
InChI=1S/C13H16N2.ClH/c1-9-5-4-6-12(10(9)2)11(3)13-7-14-8-15-13;/h4-8,11H,1-3H3,(H,14,15);1H/t11-;/m0./s1
SMILES Code
C[C@H](C1=CN=CN1)C2=CC=CC(C)=C2C.[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
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:
Dexmedetomidine is the (S)-enantiomer of medetomidine, an imidazole compound that binds to α2-adrenoceptors (Ki = 1.08 nM) with high affinity and selectivity compared to that of α1-adrenoceptors (Ki = 1.8 μM).
In vitro activity:
Primary hippocampal neurons were cultured for 8 days in vitro and pretreated with or without dexmedetomidine or phosphorylation inhibitors prior to propofol exposure. Dexmedetomidine exerts its neuroprotective effect by binding to imidazoline I1 receptors and modulating histone H3 acetylation in dopaminergic neurons in the striatum via the Erk1/2 signaling pathways. In the present study, pretreatment with dexmedetomidine evidently rescued the propofol-induced downregulation of both the BDNF mRNA (Figure 5B) and reduced levels of the p-Erk1/2, p-CREB, and BDNF proteins (Figure 6B–E). No notable difference was observed in the expression of the Erk1/2 and CREB mRNAs and proteins (Figures 5B and 6B–E) in cells pretreated with or without dexmedetomidine. In conclusion, dexmedetomidine alleviates propofol-induced cytotoxicity toward primary hippocampal neurons in vitro, which correlated with the activation of Erk1/2/CREB/BDNF signaling pathways. Reference: Drug Des Devel Ther. 2019 Feb 19;13:695-706. https://pubmed.ncbi.nlm.nih.gov/30858699/
In vivo activity:
Primary hippocampal neurons were cultured for 8 days in vitro and pretreated with or without dexmedetomidine or phosphorylation inhibitors prior to propofol exposure. Dexmedetomidine exerts its neuroprotective effect by binding to imidazoline I1 receptors and modulating histone H3 acetylation in dopaminergic neurons in the striatum via the Erk1/2 signaling pathways. In the present study, pretreatment with dexmedetomidine evidently rescued the propofol-induced downregulation of both the BDNF mRNA (Figure 5B) and reduced levels of the p-Erk1/2, p-CREB, and BDNF proteins (Figure 6B–E). No notable difference was observed in the expression of the Erk1/2 and CREB mRNAs and proteins (Figures 5B and 6B–E) in cells pretreated with or without dexmedetomidine. In conclusion, dexmedetomidine alleviates propofol-induced cytotoxicity toward primary hippocampal neurons in vitro, which correlated with the activation of Erk1/2/CREB/BDNF signaling pathways. Reference: Drug Des Devel Ther. 2019 Feb 19;13:695-706. https://pubmed.ncbi.nlm.nih.gov/30858699/
Solvent mg/mL mM
Solubility
DMSO 25.0 105.60
DMF 25.0 105.60
Ethanol 30.0 126.72
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 236.74 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. Yang XM, Liu J, Ji J, Xie J. Effects of dexmedetomidine on the deformability of erythrocytes in vitro and in anesthesia. Exp Ther Med. 2014 Jun;7(6):1631-1634. doi: 10.3892/etm.2014.1633. Epub 2014 Mar 27. PMID: 24926356; PMCID: PMC4043598. 2. Tu Y, Liang Y, Xiao Y, Lv J, Guan R, Xiao F, Xie Y, Xiao Q. Dexmedetomidine attenuates the neurotoxicity of propofol toward primary hippocampal neurons in vitro via Erk1/2/CREB/BDNF signaling pathways. Drug Des Devel Ther. 2019 Feb 19;13:695-706. doi: 10.2147/DDDT.S188436. PMID: 30858699; PMCID: PMC6387615. 3. Li J, Chen Q, He X, Alam A, Ning J, Yi B, Lu K, Gu J. Dexmedetomidine attenuates lung apoptosis induced by renal ischemiareperfusion injury through α2AR/PI3K/Akt pathway. J Transl Med. 2018 Mar 23;16(1):78. doi: 10.1186/s12967-018-1455-1. PMID: 29566706; PMCID: PMC5865375. 4. Wang Z, Wu J, Hu Z, Luo C, Wang P, Zhang Y, Li H. Dexmedetomidine Alleviates Lipopolysaccharide-Induced Acute Kidney Injury by Inhibiting p75NTR-Mediated Oxidative Stress and Apoptosis. Oxid Med Cell Longev. 2020 Oct 31;2020:5454210. doi: 10.1155/2020/5454210. PMID: 33194004; PMCID: PMC7648709.
In vitro protocol:
1. Yang XM, Liu J, Ji J, Xie J. Effects of dexmedetomidine on the deformability of erythrocytes in vitro and in anesthesia. Exp Ther Med. 2014 Jun;7(6):1631-1634. doi: 10.3892/etm.2014.1633. Epub 2014 Mar 27. PMID: 24926356; PMCID: PMC4043598. 2. Tu Y, Liang Y, Xiao Y, Lv J, Guan R, Xiao F, Xie Y, Xiao Q. Dexmedetomidine attenuates the neurotoxicity of propofol toward primary hippocampal neurons in vitro via Erk1/2/CREB/BDNF signaling pathways. Drug Des Devel Ther. 2019 Feb 19;13:695-706. doi: 10.2147/DDDT.S188436. PMID: 30858699; PMCID: PMC6387615.
In vivo protocol:
1. Li J, Chen Q, He X, Alam A, Ning J, Yi B, Lu K, Gu J. Dexmedetomidine attenuates lung apoptosis induced by renal ischemiareperfusion injury through α2AR/PI3K/Akt pathway. J Transl Med. 2018 Mar 23;16(1):78. doi: 10.1186/s12967-018-1455-1. PMID: 29566706; PMCID: PMC5865375. 2. Wang Z, Wu J, Hu Z, Luo C, Wang P, Zhang Y, Li H. Dexmedetomidine Alleviates Lipopolysaccharide-Induced Acute Kidney Injury by Inhibiting p75NTR-Mediated Oxidative Stress and Apoptosis. Oxid Med Cell Longev. 2020 Oct 31;2020:5454210. doi: 10.1155/2020/5454210. PMID: 33194004; PMCID: PMC7648709.
1: Keating GM. Dexmedetomidine: A Review of Its Use for Sedation in the Intensive Care Setting. Drugs. 2015 Jul;75(10):1119-30. doi: 10.1007/s40265-015-0419-5. PMID: 26063213. 2: Persson NDÅ, Uusalo P, Nedergaard M, Lohela TJ, Lilius TO. Could dexmedetomidine be repurposed as a glymphatic enhancer? Trends Pharmacol Sci. 2022 Dec;43(12):1030-1040. doi: 10.1016/j.tips.2022.09.007. Epub 2022 Oct 21. PMID: 36280451. 3: Barends CR, Absalom A, van Minnen B, Vissink A, Visser A. Dexmedetomidine versus Midazolam in Procedural Sedation. A Systematic Review of Efficacy and Safety. PLoS One. 2017 Jan 20;12(1):e0169525. doi: 10.1371/journal.pone.0169525. PMID: 28107373; PMCID: PMC5249234. 4: Mondardini MC, Amigoni A, Cortellazzi P, Di Palma A, Navarra C, Picardo SG, Puzzutiello R, Rinaldi L, Vitale F, Zito Marinosci G, Conti G. Intranasal dexmedetomidine in pediatrics: update of current knowledge. Minerva Anestesiol. 2019 Dec;85(12):1334-1345. doi: 10.23736/S0375-9393.19.13820-5. Epub 2019 Oct 14. PMID: 31630510. 5: Afonso J, Reis F. Dexmedetomidine: current role in anesthesia and intensive care. Rev Bras Anestesiol. 2012 Jan-Feb;62(1):118-33. doi: 10.1016/S0034-7094(12)70110-1. PMID: 22248773. 6: Eizaga Rebollar R, García Palacios MV, Fernández Riobó MC, Torres Morera LM. Dexmedetomidine and perioperative analgesia in children. Rev Esp Anestesiol Reanim (Engl Ed). 2022 Oct;69(8):487-492. doi: 10.1016/j.redare.2022.08.003. Epub 2022 Sep 10. PMID: 36100555. 7: Mahmoud M, Mason KP. Dexmedetomidine: review, update, and future considerations of paediatric perioperative and periprocedural applications and limitations. Br J Anaesth. 2015 Aug;115(2):171-82. doi: 10.1093/bja/aev226. PMID: 26170346. 8: Chima AM, Mahmoud MA, Narayanasamy S. What Is the Role of Dexmedetomidine in Modern Anesthesia and Critical Care? Adv Anesth. 2022 Dec;40(1):111-130. doi: 10.1016/j.aan.2022.06.003. PMID: 36333042. 9: Carr ZJ, Cios TJ, Potter KF, Swick JT. Does Dexmedetomidine Ameliorate Postoperative Cognitive Dysfunction? A Brief Review of the Recent Literature. Curr Neurol Neurosci Rep. 2018 Aug 6;18(10):64. doi: 10.1007/s11910-018-0873-z. PMID: 30083844. 10: Kawazoe Y, Miyamoto K, Morimoto T, Yamamoto T, Fuke A, Hashimoto A, Koami H, Beppu S, Katayama Y, Itoh M, Ohta Y, Yamamura H; Dexmedetomidine for Sepsis in Intensive Care Unit Randomized Evaluation (DESIRE) Trial Investigators. Effect of Dexmedetomidine on Mortality and Ventilator-Free Days in Patients Requiring Mechanical Ventilation With Sepsis: A Randomized Clinical Trial. JAMA. 2017 Apr 4;317(13):1321-1328. doi: 10.1001/jama.2017.2088. PMID: 28322414; PMCID: PMC5469298. 11: Duan X, Coburn M, Rossaint R, Sanders RD, Waesberghe JV, Kowark A. Efficacy of perioperative dexmedetomidine on postoperative delirium: systematic review and meta-analysis with trial sequential analysis of randomised controlled trials. Br J Anaesth. 2018 Aug;121(2):384-397. doi: 10.1016/j.bja.2018.04.046. Epub 2018 Jun 22. PMID: 30032877. 12: Coursin DB, Coursin DB, Maccioli GA. Dexmedetomidine. Curr Opin Crit Care. 2001 Aug;7(4):221-6. doi: 10.1097/00075198-200108000-00002. PMID: 11571417. 13: Jun JH, Kim KN, Kim JY, Song SM. The effects of intranasal dexmedetomidine premedication in children: a systematic review and meta-analysis. Can J Anaesth. 2017 Sep;64(9):947-961. English. doi: 10.1007/s12630-017-0917-x. Epub 2017 Jun 21. PMID: 28639236. 14: Qiu Z, Lu P, Wang K, Zhao X, Li Q, Wen J, Zhang H, Li R, Wei H, Lv Y, Zhang S, Zhang P. Dexmedetomidine Inhibits Neuroinflammation by Altering Microglial M1/M2 Polarization Through MAPK/ERK Pathway. Neurochem Res. 2020 Feb;45(2):345-353. doi: 10.1007/s11064-019-02922-1. Epub 2019 Dec 10. PMID: 31823113. 15: Poon WH, Ling RR, Yang IX, Luo H, Kofidis T, MacLaren G, Tham C, Teoh KLK, Ramanathan K. Dexmedetomidine for adult cardiac surgery: a systematic review, meta-analysis and trial sequential analysis. Anaesthesia. 2023 Mar;78(3):371-380. doi: 10.1111/anae.15947. Epub 2022 Dec 19. PMID: 36535747. 16: Mantz J, Josserand J, Hamada S. Dexmedetomidine: new insights. Eur J Anaesthesiol. 2011 Jan;28(1):3-6. doi: 10.1097/EJA.0b013e32833e266d. PMID: 20881501. 17: Burlacu CC, Neag MA, Mitre AO, Sirbu AC, Badulescu AV, Buzoianu AD. The Role of miRNAs in Dexmedetomidine's Neuroprotective Effects against Brain Disorders. Int J Mol Sci. 2022 May 13;23(10):5452. doi: 10.3390/ijms23105452. PMID: 35628263; PMCID: PMC9141783. 18: Nair AS, Saifuddin MS, Naik V, Rayani BK. Dexmedetomidine in cancer surgeries: Present status and consequences with its use. Indian J Cancer. 2020 Jul-Sep;57(3):234-238. doi: 10.4103/ijc.IJC_376_19. PMID: 32769293. 19: Vorobeichik L, Brull R, Abdallah FW. Evidence basis for using perineural dexmedetomidine to enhance the quality of brachial plexus nerve blocks: a systematic review and meta-analysis of randomized controlled trials. Br J Anaesth. 2017 Feb;118(2):167-181. doi: 10.1093/bja/aew411. PMID: 28100520. 20: Wang W, Ma Y, Liu Y, Wang P, Liu Y. Effects of Dexmedetomidine Anesthesia on Early Postoperative Cognitive Dysfunction in Elderly Patients. ACS Chem Neurosci. 2022 Aug 3;13(15):2309-2314. doi: 10.1021/acschemneuro.2c00173. Epub 2022 Jul 21. PMID: 35864562.