Art. -Nr.: HY-12719

Dexmedetomidine

(Synonyms: (+)-Medetomidine; (S)-Medetomidine)

32 Cited Publications

Kundenbewertung

Based on 32 publication(s) in Google Scholar

Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of α2-adrenoceptor, with a K_i of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects.

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Reinheit: 99.94%
CAS. Nr.: 113775-47-6
Formel: C₁₃H₁₆N₂
Molecular Weight:200.28

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Dexmedetomidine Chemical Structure

CAS. Nr.: 113775-47-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (32)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

α2-adrenergic receptor

1.08 nM (Ki)

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	1.5 nM Compound: Dexmedetomidine	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	[PMID: 21129985]

In Vitro

Medetomidine has high selectivity for α2 adrenoceptors (K_i=1.08 nM) over α1 adrenoceptors (K_i=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.

In Vivo

Medetomidine (10-100 μg/kg; i.v. at 5-min intervals) produces a dose-dependent pupillary dilatation in pentobarbitone-anaesthetized rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female Sprague-Dawley rats (270-350 g)^[1]
Dosage:

1, 5, 10, 50, 100 mg/kg
Administration:

I.v. at 5-min intervals
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

CAS. Nr. 113775-47-6
Appearance Solid
Molecular Weight 200.28
Formel C₁₃H₁₆N₂
Color White to off-white
SMILES

C[C@H](C1=CN=CN1)C2=CC=CC(C)=C2C
Synonyms

(+)-Medetomidine; (S)-Medetomidine
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

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

Glymphatic influx is negatively correlated with cerebral blood volume in male mice. [Abstract]

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
Mol Cell Toxicol

2023 Jun 2.
bioRxiv

2026 Mar 7.
University of Colorado Denver

2024.
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.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.9930 mL

24.9650 mL

49.9301 mL

5 mM

0.9986 mL

4.9930 mL

9.9860 mL

10 mM

0.4993 mL

2.4965 mL

4.9930 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 (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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (10.39 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Dexmedetomidine

32 Cited Publications

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Dexmedetomidine

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Publications Citing Use of MedChemExpress (MCE) Dexmedetomidine

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (32)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Dexmedetomidine Related Classifications

HY-12719 Related Classifications