Dexmedetomidine
Based on 32 publication(s) in Google Scholar
Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 113775-47-6
- Formula: C13H16N2
- Molecular Weight:200.28
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) Dexmedetomidine
More- Nat Commun. 2023 Jul 7;14(1):4011. [Abstract]
- Am J Chin Med. 2025;53(2):501-522. [Abstract]
- Cell Rep. 2026 Mar 28;45(4):117182. [Abstract]
- Drug Des Devel Ther. 2024 Apr 9:18:1103-1114. [Abstract]
- Cancer Metab. 2025 Jun 23;13(1):33. [Abstract]
- Sci Rep. 2025 Sep 29;15(1):33699. [Abstract]
- Mol Cell Biochem. 2026 May;481(5):2083-2095. [Abstract]
- Mol Cell Biochem. 2026 Mar 13. [Abstract]
- Brain Res Bull. 2026 Apr:237:111839. [Abstract]
- Brain Res Bull. 2025 Aug 24:230:111523. [Abstract]
- Neurochem Res. 2025 Apr 9;50(2):138. [Abstract]
- Front Biosci (Landmark Ed). 2025 Feb 20;30(2):27159. [Abstract]
- Metab Brain Dis. 2025 Nov 5;40(8):306. [Abstract]
- Hum Exp Toxicol. 2025 Jan-Dec:44:9603271251336467. [Abstract]
- Cardiovasc Drugs Ther. 2025 Feb;39(1):33-42. [Abstract]
- Hum Exp Toxicol. 2021 Dec;40(12):2145-2155. [Abstract]
- Chem Biol Drug Des. 2025 Apr;105(4):e70100. [Abstract]
- J Neuropathol Exp Neurol. 2022 Sep 19;81(10):836-849. [Abstract]
- BMC Anesthesiol. 2026 Jun 1. [Abstract]
- Brain Res. 2025 Jan 30:149482. [Abstract]
- Tissue Cell. 2026 Jun 8:103:103683. [Abstract]
- Kaohsiung J Med Sci. 2025 May 15:e70045. [Abstract]
- Dose Response. 2026 Apr 24;24(2):15593258261445031. [Abstract]
- Pharmacology. 2022;107(1-2):14-27. [Abstract]
- Eur J Neurosci. 2021 Dec;54(11):7775-7789. [Abstract]
- Histol Histopathol. 2025 Mar 28:18914. [Abstract]
- Exp Brain Res. 2026 Jun 15;244(7):135. [Abstract]
- J Toxicol Sci. 2023;48(3):139-148. [Abstract]
- Mol Cell Toxicol. 2023 Jun 2.
- bioRxiv. 2026 Mar 7.
- University of Colorado Denver. 2024.
- Biomed Pharmacother. 2023 Dec 31:169:115915. [Abstract]
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Cell Imaging/Staining
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Histological Imaging/Staining
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Bio/Physico-chemical Assay
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RT-PCR
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IF
All Adrenergic Receptor Isoforms
More
Biological Activity
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α2-adrenergic receptor 1.08 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
1.5 nM
Compound: Dexmedetomidine
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Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
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[PMID: 21129985] |
Medetomidine has high selectivity for α2 adrenoceptors (Ki=1.08 nM) over α1 adrenoceptors (Ki=1750 nM) in rat brain membranes[1].
Medetomidine (0.1-100 nM) inhibits the twitch response in field-stimulated mouse vas deferens, with a pD2 of 9.0[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Sprague-Dawley rats (270-350 g)[1]
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Dosage:1, 5, 10, 50, 100 mg/kg
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Administration:I.v. at 5-min intervals
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Result:Produced the pupil dilatation of 2.5 mm (approximately half of the maximum effect) at the cumulative dose of 4 μg/kg.
Chemical Information
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CAS No. 113775-47-6
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Appearance Solid
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Molecular Weight 200.28
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Formula C13H16N2
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Color White to off-white
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SMILES
C[C@H](C1=CN=CN1)C2=CC=CC(C)=C2C
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Synonyms
(+)-Medetomidine; (S)-Medetomidine
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (32)
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Journal Impact Factor
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Most Recent
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Nat Commun
Porous microneedle patch with sustained delivery of extracellular vesicles mitigates severe spinal cord injury. [Abstract]2023 Jul 7;14(1):4011. PMID: 37419902 -
Am J Chin Med
Ophiopogonin D from Ophiopogon japonicas-induced USP25 Activity to Reduce Ferroptosis of Macrophage in Acute Lung Injury by the Inhibition of Bound Rac1 and Nox1 Complex. [Abstract]2025;53(2):501-522. PMID: 40099394 -
Cell Rep
2026 Mar 28;45(4):117182. PMID: 41904953 -
Drug Des Devel Ther
Dexmedetomidine Prolongs Lidocaine Intravenous Regional Anesthesia in Rats by Blocking the Hyperpolarization-Activated Cation Current. [Abstract]2024 Apr 9:18:1103-1114. PMID: 38618283 -
Cancer Metab
Dexmedetomidine promotes colorectal cancer progression mediated by gamma-aminobutyric acid signaling. [Abstract]2025 Jun 23;13(1):33. PMID: 40551256 -
Sci Rep
Dexmedetomidine regulates the SIRT3-mediated JAK2/STAT3 signaling pathway to protect against sepsis-induced intestinal injury. [Abstract]2025 Sep 29;15(1):33699. PMID: 41023284 -
Mol Cell Biochem
Dexmedetomidine inhibits microglia activation, neuroinflammation, and glycolysis in postoperative cognitive dysfunction by promoting YTHDF2-mediated PKM2 mRNA degradation. [Abstract]2026 May;481(5):2083-2095. PMID: 41925799 -
Mol Cell Biochem
Decoding dexmedetomidine's multiple mechanisms in atherosclerosis: effects on lipid metabolism, inflammation, cholesterol efflux, and foam cell formation. [Abstract]2026 Mar 13. PMID: 41824202 -
Brain Res Bull
Dexmedetomidine ameliorates postoperative delirium-like behavior in aged mice by restoring microglial autophagy via MAPK14 inhibition. [Abstract]2026 Apr:237:111839. PMID: 41865902 -
Brain Res Bull
Dexmedetomidine attenuates postoperative delirium by activating Nrf2 to reduce oxidative stress and blood-brain barrier disruption. [Abstract]2025 Aug 24:230:111523. PMID: 40858194 -
Neurochem Res
Dexmedetomidine Promotes Angiogenesis After Ischemic Stroke Through the NRF2/HO-1/VEGF Pathway. [Abstract]2025 Apr 9;50(2):138. PMID: 40202562 -
Front Biosci (Landmark Ed)
Dexmedetomidine Protects the Brain: Exploring the α2AR/FAK Pathway in Post-Stroke Intestinal Barrier Repair. [Abstract]2025 Feb 20;30(2):27159. PMID: 40018945 -
Metab Brain Dis
Dexmedetomidine alleviates ferroptosis caused by traumatic brain injury via the NRF2/HO-1/GPX4 pathway. [Abstract]2025 Nov 5;40(8):306. PMID: 41191138 -
Hum Exp Toxicol
Protective effects of dexmedetomidine against propofol-induced memory impairment in developing rat involved Src and RARα. [Abstract]2025 Jan-Dec:44:9603271251336467. PMID: 40296644 -
Cardiovasc Drugs Ther
Dexmedetomidine Alleviates Abdominal Aortic Aneurysm by Activating Autophagy Via AMPK/mTOR Pathway. [Abstract]2025 Feb;39(1):33-42. PMID: 37392236 -
Hum Exp Toxicol
Protective effect of dexmedetomidine on neuronal hypoxic injury through inhibition of miR-134. [Abstract]2021 Dec;40(12):2145-2155. PMID: 34121490 -
Chem Biol Drug Des
The Role of the Sirt1/Foxo3a Pathway in Mitigating Myocardial Ischemia-Reperfusion Injury by Dexmedetomidine. [Abstract]2025 Apr;105(4):e70100. PMID: 40230274 -
J Neuropathol Exp Neurol
Dexmedetomidine Inhibits NF-κB-Transcriptional Activity in Neurons Undergoing Ischemia-Reperfusion by Regulating O-GlcNAcylation of SNW1. [Abstract]2022 Sep 19;81(10):836-849. PMID: 35818332 -
BMC Anesthesiol
Dexmedetomidine may alleviate severe acute pancreatitis-associated lung injury by targeting the AIM2 inflammasome in endothelial cells. [Abstract]2026 Jun 1. PMID: 42226110 -
Brain Res
Role of dexmedetomidine in postoperative cognitive dysfunction and sleep improvement in aged rats by regulating the PI3K/Akt signaling pathway and its mechanism. [Abstract]2025 Jan 30:149482. PMID: 39892804 -
Tissue Cell
Rosmarinic acid ameliorates radiation-induced intestinal injury through PI3K/AKT/NF-κB/MMP9 axis inhibition: From network pharmacology prediction to experimental validation. [Abstract]2026 Jun 8:103:103683. PMID: 42269422 -
Kaohsiung J Med Sci
Dexmedetomidine Blocks the ERK Pathway by Inhibiting MAP3K8 to Achieve a Protective Effect in Lung Ischemia/Reperfusion Injury. [Abstract]2025 May 15:e70045. PMID: 40372180 -
Dose Response
Dexmedetomidine Improves BBB and Neuronal Damage in Subarachnoid Hemorrhage by Repressing S100A4-Mediated Astrocytic Reactivity. [Abstract]2026 Apr 24;24(2):15593258261445031. PMID: 42064389 -
Pharmacology
Dexmedetomidine Attenuates Hypoxia/Reoxygenation Injury of H9C2 Myocardial Cells by Upregulating miR-146a Expression via the MAPK Signal Pathway. [Abstract]2022;107(1-2):14-27. PMID: 34718238 -
Eur J Neurosci
Dexmedetomidine attenuates propofol-induced apoptosis of neonatal hippocampal astrocytes by inhibiting the Bcl2l1 signalling pathway. [Abstract]2021 Dec;54(11):7775-7789. PMID: 34734676 -
Histol Histopathol
The mechanism of dexmedetomidine regulation of the HIF-1α/FUNDC1 axis in myocardial ischemia/reperfusion injury. [Abstract]2025 Mar 28:18914. PMID: 40235277 -
Exp Brain Res
Dexmedetomidine inhibits microglia ferroptosis to relieve postoperative cognitive dysfunction in elderly rats through JPX/HIF-1/DHODH pathway. [Abstract]2026 Jun 15;244(7):135. PMID: 42295409 -
J Toxicol Sci
Dexmedetomidine protects against Ropivacaine-induced neuronal pyroptosis via the Nrf2/HO-1 pathway. [Abstract]2023;48(3):139-148. PMID: 36858639 -
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Biomed Pharmacother
Dexmedetomidine alleviates ferroptosis following hepatic ischemia-reperfusion injury by upregulating Nrf2/GPx4-dependent antioxidant responses. [Abstract]2023 Dec 31:169:115915. PMID: 38000361
Dexmedetomidine purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2023 Dec 31:169:115915. [Abstract]
Dexmedetomidine (Dex) (10 nM; 24 h) treatment significantly reduced the number of AML12 cells damaged via OGD/R.
Dexmedetomidine purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2023 Dec 31:169:115915. [Abstract]
Dexmedetomidine (Dex) (50 mg/kg; i.p.) treatment significantly ameliorated the hepatic pathological changes in the HIRI mice.
Dexmedetomidine purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2023 Dec 31:169:115915. [Abstract]
Dexmedetomidine (Dex) (50 mg/kg; i.p.) treatment significantly reduced ALT and AST levels in the HIRI model mice.
Dexmedetomidine purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2023 Dec 31:169:115915. [Abstract]
Dexmedetomidine (Dex) (10 nM; 24 h) increased GPX4 and SLC7A11 mRNA levels in OGD/R-induced AML12 cells.
Dexmedetomidine purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2023 Dec 31:169:115915. [Abstract]
Dexmedetomidine (Dex) (10 nM; 24 h) significantly increased the protein expression and nuclear levels of Nrf2 in OGD/R-treated AML12 cells.
Solvent & Solubility
DMSO : 125 mg/mL (624.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (10.39 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (10.39 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Virtanen R, et, al. Characterization of the selectivity, specificity and potency of medetomidine as an alpha 2-adrenoceptor agonist. Eur J Pharmacol. 1988 May 20;150(1-2):9-14. [Content Brief]
[2]. Gertler R, et, al. Dexmedetomidine: a novel sedative-analgesic agent. Proc (Bayl Univ Med Cent). 2001 Jan;14(1):13-21. [Content Brief]
[3]. Sajid B, et, al. A comparison of oral dexmedetomidine and oral midazolam as premedicants in children. J Anaesthesiol Clin Pharmacol. Jan-Mar 2019;35(1):36-40. [Content Brief]
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.9930 mL | 24.9650 mL | 49.9301 mL | 124.8252 mL |
| 5 mM | 0.9986 mL | 4.9930 mL | 9.9860 mL | 24.9650 mL | |
| 10 mM | 0.4993 mL | 2.4965 mL | 4.9930 mL | 12.4825 mL | |
| 15 mM | 0.3329 mL | 1.6643 mL | 3.3287 mL | 8.3217 mL | |
| 20 mM | 0.2497 mL | 1.2483 mL | 2.4965 mL | 6.2413 mL | |
| 25 mM | 0.1997 mL | 0.9986 mL | 1.9972 mL | 4.9930 mL | |
| 30 mM | 0.1664 mL | 0.8322 mL | 1.6643 mL | 4.1608 mL | |
| 40 mM | 0.1248 mL | 0.6241 mL | 1.2483 mL | 3.1206 mL | |
| 50 mM | 0.0999 mL | 0.4993 mL | 0.9986 mL | 2.4965 mL | |
| 60 mM | 0.0832 mL | 0.4161 mL | 0.8322 mL | 2.0804 mL | |
| 80 mM | 0.0624 mL | 0.3121 mL | 0.6241 mL | 1.5603 mL | |
| 100 mM | 0.0499 mL | 0.2497 mL | 0.4993 mL | 1.2483 mL |