Medetomidine

Cat. No.: HY-17034 Purity: 99.99%: FAQs
Data Sheet SDS COA Handling Instructions

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Medetomidine is an orally active α2-adrenoceptor agonist (K_i: 1.08 nM). Medetomidine has sedative and analgesic effects. Medetomidine can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels.

For research use only. We do not sell to patients.

Medetomidine Chemical Structure

CAS No. : 86347-14-0

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
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α adrenergic receptor β adrenergic receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

α2-adrenergic receptor

1.08 nM (Ki)

α1-adrenergic receptor

1750 nM (Ki)

In Vitro

Medetomidine (0-1 µM, 1 h) inhibits aldosterone release from the adrenocortical cell suspension^[7].
Medetomidine (10 nM) activates a kicking response in Cyprids^[8].
Medetomidine (1 µM) increases cellular cAMP production by activating β-like receptors in CHO cells^[8].

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

In Vivo

Medetomidine (200 μg/kg, p.o. or i.m.) induces a sedation in cats^[4].
Medetomidine (20 µg/kg, i.v.) shows sedative and analgesic effects in dogs^[5].
Medetomidine (0.05-0.3 mg/kg, s.c.) protects against Diazinon-induced toxicosis in mice^[6].

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

Animal Model:	Diazinon (75 mg/kg, orally)-induced toxicosis in mice^[6]
Dosage:	0.05, 0.1 and 0.3 mg/kg
Administration:	Subcutaneous injection (s.c.), 15 min before Diazinon.
Result:	Protected the mice from the toxicity induced by Diazinon. Decreased the occurrence of Straub tail, excessive salivation and tremor. Increased the latencies to onset of tremor and death when compared with control.

Animal Model:	Dogs^[5]
Dosage:	20 µg/kg
Administration:	Intravenous injection (i.v.)
Result:	Showed sedative and analgesic effects. Increased in SAP, MAP, DAP, MPAP, PCWP, CVP, SVR, PVR, core body temperature. Decreased in HR, CO, CI, SV, SI, RR, pH.

Molecular Weight

200.28

Formula

C₁₃H₁₆N₂

CAS No.

86347-14-0

Appearance

Solid

Color

White to off-white

SMILES

CC(C1=CN=CN1)C2=CC=CC(C)=C2C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (1248.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (12.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (12.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (12.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.99%

Select Batch:

Data Sheet (282 KB) SDS (0 KB)

COA (254 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief]

[2]. Kallio A, et al. Acute effects of medetomidine, a selective alpha 2-adrenoceptor agonist, on anterior pituitary hormone and cortisol secretion in man. Acta Endocrinol (Copenh). 1988 Sep;119(1):11-5. [Content Brief]

[3]. R Virtanen, et al. Characterization of the selectivity, specificity and potency of medetomidine as an a2-adrenoceptor agonist. [Content Brief]

[4]. O. B. Ansah, et al. Comparing oral and intramuscular administration of medetomidine in cats.

[5]. Kuo WC, et al. Comparative cardiovascular, analgesic, and sedative effects of medetomidine, medetomidine-hydromorphone, and medetomidine-butorphanol in dogs. Am J Vet Res. 2004 Jul;65(7):931-7. [Content Brief]

[6]. Yakoub LK, et al. Medetomidine protection against diazinon-induced toxicosis in mice. Toxicol Lett. 1997 Sep 19;93(1):1-8. [Content Brief]

[7]. Jager LP, et al. Effects of atipamezole, detomidine and medetomidine on release of steroid hormones by porcine adrenocortical cells in vitro. Eur J Pharmacol. 1998 Apr 3;346(1):71-6. [Content Brief]

[8]. Ulrika Lind, et al. Octopamine receptors from the barnacle balanus improvisus are activated by the alpha2-adrenoceptor agonist medetomidine. [Content Brief]

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

Medetomidine Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Medetomidine86347-14-0Adrenergic ReceptorBeta ReceptorSedativeanalgesicvasoconstrictionaldosteronecAMPCHOtoxicosisInhibitorinhibitorinhibit

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