Vatinoxan hydrochloride
Based on 3 publication(s) in Google Scholar
Vatinoxan hydrochloride (MK-467 hydrochloride) is a peripherally selective α2-Adrenoceptor antagonist. Vatinoxan hydrochloride blocks peripheral α2-adrenoceptor-mediated vasoconstriction, bradycardia, hyperglycemia, diuresis, lens opacity, and decreased intraocular pressure, delays pupil dilation, and maintains corneal thickness. Vatinoxan hydrochloride, 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.
For research use only. We do not sell to patients.
- Purity : 99.79%
- CAS No.: 130466-38-5
- Formula: C20H27ClN4O4S
- Molecular Weight:454.97
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Storage:
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Vatinoxan hydrochloride
MoreAll Adrenergic Receptor Isoforms
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Biological Activity
Description
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. 130466-38-5
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Appearance Solid
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Molecular Weight 454.97
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Formula C20H27ClN4O4S
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Color White to light yellow
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SMILES
[H]Cl.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 hydrochloride; L-659066 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
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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Solvent & Solubility
In Vitro:
DMSO : 10 mg/mL (21.98 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 (stored under nitrogen, away from moisture). 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 (stored under nitrogen, away from moisture). 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)
Purity & Documentation
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Data Sheet (293 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (stored under nitrogen, away from moisture). 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 | 2.1979 mL | 10.9897 mL | 21.9795 mL | 54.9487 mL |
| 5 mM | 0.4396 mL | 2.1979 mL | 4.3959 mL | 10.9897 mL | |
| 10 mM | 0.2198 mL | 1.0990 mL | 2.1979 mL | 5.4949 mL | |
| 15 mM | 0.1465 mL | 0.7326 mL | 1.4653 mL | 3.6632 mL | |
| 20 mM | 0.1099 mL | 0.5495 mL | 1.0990 mL | 2.7474 mL |
Vatinoxan hydrochloride Related Classifications
HY-19057A Related Classifications
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