Vatinoxan
Based on 3 publication(s) in Google Scholar
Vatinoxan (MK-467) is a peripherally selective α2-Adrenoceptor antagonist. Vatinoxan blocks peripheral α2-adrenoceptor-mediated vasoconstriction, bradycardia, hyperglycemia, diuresis, lens opacity, and decreased intraocular pressure, delays pupil dilation, and maintains corneal thickness. Vatinoxan, when combined with Medetomidine (HY-17034)/benzodiazepines, reduces respiratory rate and increases pulse rate, cutaneous microcirculation, tissue oxygenation, peripheral heat loss, and cardiac index, while altering gastrointestinal perfusion and mean arterial pressure, without causing death, hypotension, or hypoglycemia, and blocks vasoconstriction of chelonian resistance arteries.
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- Purity : 99.83%
- CAS No.: 114914-42-0
- 화학식: C20H26N4O4S
- 분자량:418.51
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Vatinoxan
MoreAll Adrenergic Receptor Isoforms
More
Biological Activity
제품 설명
IC50 & Target
[1]|
α2-adrenergic receptor |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 12-14 weeks of age, 358-418 g; n = 9 in MM-V group)[1]
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Dosage:8 mg/kg
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Administration:subcutaneous; once
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Result:Globe position grade was lower in MM-V than MM at 10 min and lower than MM and MM-I at 50 min.
Globe exposure ratio was lower in MM-V than MM at 10 min and lower than MM and MM-I at 50 min.
Lenticular opacities were almost absent in MM-V and were less severe than in MM at 30 min and than in MM and MM-I at 50 min.
Mydriasis occurred later in MM-V than MM.
Corneal opacities were grade 2 in all but two animals; one MM-V animal had grade 3.
Corneal edema was not detected in any animal.
No corneal ulcers were detected.
CCT was higher in MM-V than MM at 30 and 50 min.
Blood glucose did not change over time in MM-V.
AHG was lower in MM-V than MM.
Rectal temperatures did not differ between groups or time points.
Baseline IOP averaged 12.1 mmHg without group differences.
IOP decreased after all administrations, but the early decline was blunted in MM-V.
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Animal Model:Wistar (adult; 10 male and 2 female; 256-506 g)[3]
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Dosage:5.0 mg/kg
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Administration:subcutaneous; once
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Result:Onset of sedation was 5.35 min.
Loss of righting reflex was 6.53 min.
Blood glucose concentration at 30 min was 11.8 mmol/L; highest individual blood glucose was 13.8 mmol/L.
Spontaneous urinary voiding was 0.9 mL/kg/h (median, range 0-8.0).
Heart rate at 10, 20, and 30 min was 318, 278, and 255 beats/min.
SpO2 at 10, 20, and 30 min was 90%, 90%, and 88%.
Respiratory rate at 10, 20, and 30 min was 67, 59, and 53 breaths/min.
Rectal temperature at 10, 20, and 30 min was 36.8°C, 36.7°C, and 36.4°C.
Skin colour score at 10, 20, and 30 min was 2, 2.5, and 2.5, where 1 = pale, 2 = normal, 3 = hyperaemic.
Pelvic limb nociceptive withdrawal reflex was present during the entire postinjection period in one rat.
None of the rats had righting reflex 10 minutes after vatinoxan.
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Animal Model:Hsd:Sprague-Dawley (female; 190-270 g)[4]
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Dosage:Vatinoxan 2, 4, or 8 mg/kg s.c.; dexmedetomidine 0.2 mg/kg s.c.; saline 1 mL/kg s.c.
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Administration:s.c.; single administration; at least 7 days between sessions
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Result:Exhibited no influence on EEG delta (0.5-4.5 Hz), theta (6-9 Hz), sigma (10-15 Hz), or beta (15-30 Hz) power during the 180 min recording at any dose.
Dexmedetomidine induced a marked hyperglycemic response, which was prevented by vatinoxan at 4 and 8 mg/kg.
Vatinoxan prevented dexmedetomidine-induced weight loss at all doses in a dose-dependent manner.
Each vatinoxan dose (2, 4, 8 mg/kg) lowered peripheral vasoconstriction, measured as tail blood flow.
Compared with dexmedetomidine + saline, vatinoxan 2 mg/kg produced higher mean arterial pressure and systolic blood pressure at 80 min; vatinoxan 4 mg/kg had no effect on blood pressure; vatinoxan 8 mg/kg lowered mean arterial pressure, systolic blood pressure, and diastolic blood pressure at 30 min.
Vatinoxan 4 mg/kg was selected as the optimal dose for preventing peripheral effects without influencing slow-wave activity.
Chemical Information
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CAS No. 114914-42-0
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Appearance Solid
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분자량 418.51
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화학식 C20H26N4O4S
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Color White to off-white
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SMILES
CS(=O)(NCCN([C@]1(CN2)CCN3CCC4=C(OC5=CC=CC=C54)[C@]3([H])C1)C2=O)=O
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Synonyms
MK-467; L-659066
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Pain
Ethological profiling defines pain behaviors and parses analgesia from drug side effects in a mouse model of complex regional pain syndrome. [Abstract]2026 Jun 1;167(6):1453-1469. PMID: 42133564 -
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용액&용해도
In Vitro:
DMSO : 100 mg/mL (238.94 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. 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. 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.97 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.97 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.
In Vivo Dissolution Calculator
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.
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.
순도&문서
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Data Sheet (295 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
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. 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 | 2.3894 mL | 11.9471 mL | 23.8943 mL | 59.7357 mL |
| 5 mM | 0.4779 mL | 2.3894 mL | 4.7789 mL | 11.9471 mL | |
| 10 mM | 0.2389 mL | 1.1947 mL | 2.3894 mL | 5.9736 mL | |
| 15 mM | 0.1593 mL | 0.7965 mL | 1.5930 mL | 3.9824 mL | |
| 20 mM | 0.1195 mL | 0.5974 mL | 1.1947 mL | 2.9868 mL | |
| 25 mM | 0.0956 mL | 0.4779 mL | 0.9558 mL | 2.3894 mL | |
| 30 mM | 0.0796 mL | 0.3982 mL | 0.7965 mL | 1.9912 mL | |
| 40 mM | 0.0597 mL | 0.2987 mL | 0.5974 mL | 1.4934 mL | |
| 50 mM | 0.0478 mL | 0.2389 mL | 0.4779 mL | 1.1947 mL | |
| 60 mM | 0.0398 mL | 0.1991 mL | 0.3982 mL | 0.9956 mL | |
| 80 mM | 0.0299 mL | 0.1493 mL | 0.2987 mL | 0.7467 mL | |
| 100 mM | 0.0239 mL | 0.1195 mL | 0.2389 mL | 0.5974 mL |
Vatinoxan Related Classifications
HY-19057 Related Classifications
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