| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Vatinoxan hydrochloride targets α2 adrenergic receptors, specifically the peripheral α2-adrenoceptors. α2 adrenergic receptors are G protein-coupled receptors that mediate the effects of norepinephrine and epinephrine. They are classified into three subtypes: α2A, α2B, and α2C. Vatinoxan hydrochloride is a potent and selective α2-adrenoceptor antagonist with an IC50 of 3 nM against the binding of [3H]rauwolscine to rat cerebrocortical membranes. The compound is selective over α1-adrenoceptors. Vatinoxan mainly acts on peripheral α2-adrenoceptors, which distinguishes it from centrally acting α2 antagonists.
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| ln Vitro |
Vatinoxan hydrochloride demonstrates potent in vitro activity as an α2 adrenergic receptor antagonist. The compound has an IC50 of 3 nM against the binding of [3H]rauwolscine to rat cerebrocortical membranes, indicating high affinity for α2-adrenoceptors. Vatinoxan is selective over α1-adrenoceptors. The compound's potent and selective peripheral α2 antagonism makes it a valuable tool for studying the role of peripheral α2 adrenergic receptors in various physiological processes, including cardiovascular function, sedation, and analgesia. The compound's peripheral selectivity minimizes central nervous system effects that are often associated with α2 antagonists that cross the blood-brain barrier.
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| ln Vivo |
By alone, vitexan improves tissue oxygen delivery and cardiac index without having any negative side effects. In dogs that were awake, vatinoxan had no effect on pulmonary outcomes, but it did, in a dose-dependent manner, reduce or prevent the systemic hemodynamic effects of dexmedetomidine when given concurrently intravenously. Cardiovascular function is not significantly affected by a dose ratio of 50:1 (Vatinoxan:dexmedetomidine) [1]. Without affecting the sedative effect's quality, vatinoxan reduces the bradycardia brought on by dexmedetomidine in a dose-dependent manner. When administered to awake cats receiving dexmedetomidine, vatinoxan may help mitigate the reduction in heart rate [2].
In vivo, Vatinoxan hydrochloride has been studied for its effects on peripheral α2 adrenergic receptor-mediated functions. The compound mainly acts on peripheral α2-adrenoceptors. By blocking peripheral α2 receptors, Vatinoxan can modulate cardiovascular responses, reduce sedation, and counteract the peripheral effects of α2 agonists such as medetomidine and dexmedetomidine. The compound's peripheral selectivity allows for the study of peripheral α2 receptor functions without central effects. Detailed in vivo efficacy data, including specific model results and dosing regimens, are available in the primary literature. Vatinoxan hydrochloride is a valuable tool for studying peripheral α2 adrenergic receptor pharmacology. |
| Enzyme Assay |
The in vitro receptor binding assay for Vatinoxan hydrochloride measures the compound's affinity for α2 adrenergic receptors. Membrane preparations from rat cerebrocortical membranes or cells expressing human α2 adrenergic receptor subtypes are incubated with varying concentrations of Vatinoxan hydrochloride in the presence of a radiolabeled α2 receptor ligand such as [3H]rauwolscine. The amount of bound radioligand is measured by scintillation counting, and IC50 and Ki values are determined by fitting competition binding curves. The IC50 value of 3 nM is determined against the binding of [3H]rauwolscine to rat cerebrocortical membranes. The compound is dissolved in DMSO and diluted in assay buffer. Selectivity is assessed by testing the compound against α1-adrenoceptors and other receptor targets. Appropriate positive controls and negative controls are included in each assay run.
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| Cell Assay |
The in vitro functional assay for Vatinoxan hydrochloride measures the compound's antagonist activity at α2 adrenergic receptors. Cells expressing α2 adrenergic receptor subtypes are treated with varying concentrations of Vatinoxan hydrochloride or vehicle control (DMSO) prior to stimulation with an α2 agonist such as clonidine or UK-14304. α2 receptor activation is measured by assessing downstream signaling events such as inhibition of cAMP accumulation (α2 receptors are Gi-coupled). The reversal of agonist-induced inhibition of cAMP accumulation by Vatinoxan is quantified, and antagonist potency (IC50 or KB) is determined. The compound's selectivity for peripheral α2 receptors over central α2 receptors can be assessed using different receptor subtypes or tissue preparations.
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| Animal Protocol |
In vivo animal experiments with Vatinoxan hydrochloride are conducted using rodent models to assess the compound's effects on peripheral α2 adrenergic receptor-mediated functions. Vatinoxan is administered via intravenous, intraperitoneal, or subcutaneous injection. The compound's ability to block peripheral α2 receptor-mediated effects such as vasoconstriction, bradycardia, and sedation is assessed. The compound's effects on cardiovascular parameters (blood pressure, heart rate) are measured. The compound's peripheral selectivity is confirmed by comparing its effects to centrally acting α2 antagonists. Detailed experimental protocols, including dosing regimens and endpoints, are described in the primary literature.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic (PK) parameters for Vatinoxan hydrochloride are not extensively documented in publicly available sources. The compound has a molecular weight of 454.97 and a chemical formula of C20H27ClN4O4S. Vatinoxan hydrochloride is soluble in DMSO for formulation purposes. For in vivo administration, the compound is typically formulated using appropriate vehicles to ensure adequate solubility and stability. The compound should be stored under conditions recommended by the manufacturer to maintain stability and prevent degradation. Detailed PK parameters including half-life, clearance, volume of distribution, and maximum concentration (Cmax) are available in the primary literature and should be consulted for specific experimental planning.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for Vatinoxan hydrochloride are not extensively documented in publicly available sources. As a research-grade compound, Vatinoxan hydrochloride is intended for laboratory research purposes only and is not approved for human therapeutic use. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment and working in a well-ventilated area. The compound should be stored according to the manufacturer's recommendations to maintain stability and prevent degradation. Comprehensive toxicological profiling (e.g., LD50, maximum tolerated dose, organ-specific toxicity) is not available from the current search results and would require consultation of the primary literature or safety data sheets.
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| References |
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| Additional Infomation |
See also: Vatinoxan (contains active ingredients)... See more...
Vatinoxan hydrochloride is a research compound developed for studying the role of peripheral α2 adrenergic receptors in cardiovascular function, sedation, and analgesia. The compound is a potent and selective peripheral α2 adrenergic receptor antagonist with an IC50 of 3 nM against rat α2 receptors and selectivity over α1 receptors. Vatinoxan is also known as MK-467 hydrochloride and L-659066 hydrochloride. The compound's peripheral selectivity makes it a valuable tool for dissecting peripheral versus central α2 receptor functions. Vatinoxan hydrochloride is not currently in clinical trials nor approved for therapeutic use; it remains an investigational tool compound for preclinical pharmacology research. Vatinoxan hydrochloride is available from various chemical suppliers for research purposes. |
| Molecular Formula |
C20H27CLN4O4S
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|---|---|
| Molecular Weight |
454.9708
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| Exact Mass |
454.144
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| CAS # |
130466-38-5
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| Related CAS # |
114914-42-0;130466-38-5 (HCl);
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| PubChem CID |
182976
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| Appearance |
White to off-white solid powder
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| LogP |
3.228
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
756
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CS(=O)(=O)NCCN1C(=O)NC[C@]12CCN3CCC4=C([C@@H]3C2)OC5=CC=CC=C45.Cl
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| InChi Key |
UTMOWVIYZQWJHT-VASSOYJASA-N
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| InChi Code |
InChI=1S/C20H26N4O4S.ClH/c1-29(26,27)22-8-11-24-19(25)21-13-20(24)7-10-23-9-6-15-14-4-2-3-5-17(14)28-18(15)16(23)12-20;/h2-5,16,22H,6-13H2,1H3,(H,21,25);1H/t16-,20+;/m0./s1
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| Chemical Name |
N-[2-[(2R,12bS)-2'-oxospiro[1,3,4,6,7,12b-hexahydro-[1]benzofuro[2,3-a]quinolizine-2,5'-imidazolidine]-1'-yl]ethyl]methanesulfonamide;hydrochloride
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| Synonyms |
MK-467 hydrochloride; MK467 hydrochloride;MK 467 hydrochloride; L-659066 hydrochloride; L659066 hydrochloride; L659066 hydrochloride; MK-467 HCl
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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 (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
DMSO : ~10 mg/mL (~21.98 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1979 mL | 10.9897 mL | 21.9795 mL | |
| 5 mM | 0.4396 mL | 2.1979 mL | 4.3959 mL | |
| 10 mM | 0.2198 mL | 1.0990 mL | 2.1979 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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