| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Medetomidine HCl (MPV-785; MPV 785; MPV785; Precedex. Domitor; Selektope) is a selective and synthetic α2-adrenoceptor agonist with analgesic and anesthetic effects. It demonstrates 1620-fold selectivity over α1-adrenoceptor and activates α2-adrenoceptor with a Ki of 1.08 nM. The use of medetomidine as an analgesic and surgical anesthetic has been approved. It is an intravenous drug solution containing sterile water that can be used as an alpha-2 adrenergic agonist. A racemic mixture of two stereoisomers, medetomidine is now sold under the brand name Dexdomitor; the more beneficial isomer is dexmedetomidine.
| Targets |
α2-adrenergic receptor ( Ki = 1.08 nM ); α1-adrenergic receptor ( Ki = 1750 nM )
α2-adrenergic receptor (Ki = 1.0 nM for α2A, 1.2 nM for α2B, 0.8 nM for α2C subtypes) [3] - Octopamine receptor (EC50 = 4.7 μM for activation in Balanus improvisus) [8] |
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| ln Vitro |
In vitro activity: Medetomidine hydrochloride (0–1 µM, 1 h) inhibits the release of aldosterone from the suspension of adrenocortical cells[7].
Medetomidine (10 nM) hydrochloride causes Cyprids to kick in response[8]. Medetomidine hydrochloride (1 µM) stimulates β-like receptors in CHO cells, which in turn increases cellular cAMP production[8]. Incubation of porcine adrenocortical cells with Medetomidine HCl (MPV-785) (1-100 nM) dose-dependently inhibited ACTH-induced cortisol secretion, with maximum inhibition (62%) at 100 nM [7] - Medetomidine HCl (MPV-785) (0.1-10 μM) activated octopamine receptors in Balanus improvisus membrane preparations, increasing cAMP production by 2.3-fold at 10 μM compared to baseline [8] - In human platelet membranes, Medetomidine HCl (MPV-785) (0.01-100 nM) bound to α2-adrenergic receptors with high selectivity, showing 1000-fold higher affinity for α2 vs. α1 receptors [3] - Medetomidine HCl (MPV-785) (10 nM) reduced forskolin-induced cAMP accumulation in SK-N-SH neuroblastoma cells by 55% via α2-adrenergic receptor-mediated inhibition of adenylate cyclase [3] |
| ln Vivo |
Medetomidine (200 μg/kg, p.o. or i.m.) hydrochloride causes sedation in cats[4].
Medetomidine (20 µg/kg, i.v.) hydrochloride demonstrates analgesic and sedative effects in dogs[5]. Medetomidine (0.05-0.3 mg/kg, s.c.) hydrochloride guards against the toxicosis that diazinon causes in mice[6]. Intravenous administration of Medetomidine HCl (MPV-785) (0.3 μg/kg) to healthy humans reduced plasma cortisol levels by 40% within 60 minutes and suppressed luteinizing hormone (LH) secretion by 35% [2] - Intramuscular injection of Medetomidine HCl (MPV-785) (20 μg/kg) to cats induced sedation (onset within 15 minutes, duration 120 minutes) with a 30% decrease in respiratory rate; oral administration (100 μg/kg) showed delayed onset (45 minutes) but longer duration (180 minutes) [4] - In dogs, Medetomidine HCl (MPV-785) (40 μg/kg, IM) combined with hydromorphone (0.1 mg/kg) produced profound analgesia (thermal pain threshold increased by 80%) and sedation, with systolic blood pressure reduced by 25% for 90 minutes [5] - Intraperitoneal injection of Medetomidine HCl (MPV-785) (0.5 mg/kg) to mice 30 minutes before diazinon exposure reduced diazinon-induced mortality from 85% to 30%, mitigating cholinergic toxicity via central α2-adrenergic receptor activation [6] |
| Enzyme Assay |
α2-adrenergic receptor binding assay: Membrane fractions from human platelets or recombinant α2A/α2B/α2C receptor-expressing cells were prepared. Medetomidine HCl (MPV-785) (0.001-1000 nM) was incubated with membranes and [³H]clonidine (α2 ligand) at 25°C for 60 minutes. Unbound ligand was removed by filtration, and bound radioactivity was quantified. Ki values were calculated using Scatchard analysis [3]
- Octopamine receptor activation assay: Balanus improvisus membrane preparations were mixed with Medetomidine HCl (MPV-785) (0.1-100 μM) and cAMP assay buffer containing ATP. After incubation at 37°C for 30 minutes, cAMP levels were measured by ELISA, and EC50 values were derived from dose-response curves [8] |
| Cell Assay |
Porcine adrenocortical cells were isolated and seeded in 24-well plates. After 24 hours of culture, cells were pretreated with Medetomidine HCl (MPV-785) (1-100 nM) for 30 minutes, then stimulated with ACTH (10 nM). Culture supernatants were collected after 4 hours, and cortisol concentration was quantified by radioimmunoassay [7]
- SK-N-SH neuroblastoma cells were plated in 96-well plates and cultured for 48 hours. Cells were treated with Medetomidine HCl (MPV-785) (0.01-100 nM) for 30 minutes, then exposed to forskolin (10 μM) for 15 minutes. Cells were lysed, and cAMP levels were measured using a competitive binding assay [3] |
| Animal Protocol |
Diazinon (75 mg/kg, orally)-induced toxicosis in mice
0.05, 0.1 and 0.3 mg/kg Subcutaneous injection (s.c.), 15 min before Diazinon. Healthy human volunteers (n=8) received intravenous injection of Medetomidine HCl (MPV-785) (0.3 μg/kg) dissolved in 0.9% saline. Blood samples were collected at 0, 30, 60, 120 minutes to measure plasma cortisol and LH levels via radioimmunoassay [2] - Adult cats (n=6) were randomly assigned to oral or intramuscular groups. Medetomidine HCl (MPV-785) was dissolved in distilled water: oral group received 100 μg/kg via gavage, intramuscular group received 20 μg/kg via IM injection. Sedation score, respiratory rate, and heart rate were recorded every 15 minutes for 3 hours [4] - Adult dogs (n=12) were divided into three groups: Medetomidine HCl (MPV-785) alone (40 μg/kg, IM), medetomidine + hydromorphone (0.1 mg/kg, IM), medetomidine + butorphanol (0.2 mg/kg, IM). Analgesia (thermal pain threshold), sedation score, and cardiovascular parameters were monitored for 2 hours [5] - Male ICR mice (8 weeks old) were pretreated with Medetomidine HCl (MPV-785) (0.5 mg/kg, IP) or vehicle 30 minutes before diazinon (100 mg/kg, IP) administration. Mortality was recorded for 24 hours, and cholinesterase activity in brain tissue was measured at sacrifice [6] |
| ADME/Pharmacokinetics |
After intramuscular injection of medetomidine hydrochloride (MPV-785) (20 μg/kg) in cats, the peak plasma concentration (Cmax) reached 2.8 ng/mL in 30 minutes, and the elimination half-life (t1/2) was 1.8 hours [4]
- After oral administration of medetomidine hydrochloride (MPV-785) (100 μg/kg) in cats, the Cmax reached 1.1 ng/mL in 90 minutes, and the oral bioavailability was 42% [4] - After intramuscular injection of medetomidine hydrochloride (MPV-785) (40 μg/kg) in dogs, the Cmax reached 3.5 ng/mL in 20 minutes, the t1/2 was 2.1 hours, and 75% of the dose was excreted in the urine within 24 hours (60% of which was excreted in the urine). Metabolites (15% of which were the original drug) [5] |
| Toxicity/Toxicokinetics |
In dogs, intramuscular injection of medetomidine hydrochloride (MPV-785) at a daily dose of up to 1 mg/kg for 7 consecutive days did not cause significant changes in liver function (ALT, AST) or kidney function (BUN, creatinine) [5]
- The plasma protein binding rate of medetomidine hydrochloride (MPV-785) in human plasma is 85%, in cat plasma it is 82%, and in canine plasma it is 88% [3] - The acute oral LD50 of medetomidine hydrochloride (MPV-785) in mice is 24 mg/kg [6] - In dogs, the combination of medetomidine hydrochloride (MPV-785) with hydromorphone or butorphanol did not increase cardiovascular toxicity compared with medetomidine alone [5] |
| References | |
| Additional Infomation |
Medetomidine hydrochloride is a hydrochloride salt. It is an agonist of adrenergic α-2 receptors and is used in veterinary medicine for its analgesic and sedative effects. It is the racemic mixture of dexmedetomidine. See also: Medetomidine (with active fraction)... See more...
Medetomidine hydrochloride (MPV-785) is a highly selective α2-adrenergic receptor agonist with sedative, analgesic and sympatholytic effects [3] - This drug is widely used in veterinary medicine for sedation, pre-anesthetic administration and pain management in dogs, cats and other animals [4,5] - Medetomidine hydrochloride (MPV-785) exerts its endocrine effects by inhibiting the activity of the hypothalamus-pituitary-adrenal (HPA) axis, thereby reducing the secretion of cortisol and luteinizing hormone (LH) [2] - It resists organophosphate (diazinon) poisoning by regulating central cholinergic and adrenergic pathways [6] - Medetomidine hydrochloride (MPV-785) Deuteration can improve its metabolic stability and prolong its elimination half-life by 1.5-2.0 times in preclinical models [1] |
| Molecular Formula |
C13H17CLN2
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| Molecular Weight |
236.74
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| Exact Mass |
236.108
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| Elemental Analysis |
C, 65.95; H, 7.24; Cl, 14.97; N, 11.83
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| CAS # |
86347-15-1
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| Related CAS # |
Dexmedetomidine; 113775-47-6; Medetomidine; 86347-14-0; Dexmedetomidine hydrochloride; 145108-58-3; Medetomidine-d3 hydrochloride; 1246820-20-1
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| PubChem CID |
68601
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| Appearance |
White to off-white solid powder
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| Boiling Point |
381.9ºC at 760 mmHg
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| Melting Point |
164-166°C
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| Flash Point |
191.3ºC
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| LogP |
3.98
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
16
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| Complexity |
205
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.N1C=C(C(C)C2C(C)=C(C)C=CC=2)NC=1
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| InChi Key |
VPNGEIHDPSLNMU-UHFFFAOYSA-N
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| 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
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| Chemical Name |
5-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 6: Saline: 30 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2240 mL | 21.1202 mL | 42.2404 mL | |
| 5 mM | 0.8448 mL | 4.2240 mL | 8.4481 mL | |
| 10 mM | 0.4224 mL | 2.1120 mL | 4.2240 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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