Rivanicline hemioxalate
Based on 1 publication(s) in Google Scholar
Rivanicline (RJR-2403) hemioxalate is a neuronal nicotinic receptor agonist. Rivanicline hemioxalate is highly selective for the rat brain cortex nAChRs (Ki = 26 nM, EC50 of 732 nM) and α4β2 subtype (Ki = 26 nM, EC50 = 16 μM). Rivanicline hemioxalate can significantly restore the learning impairment and cognitive dysfunction. Rivanicline hemioxalate can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease).
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- Reinheit: 99.78%
- Formel: C11H15N2O2
- Molecular Weight:207.23
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) Rivanicline hemioxalate
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Biologische Aktivität
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α4β2 16 μM (EC50) |
α4β4 50 μM (EC50) |
α3β2 150 μM (EC50) |
α7 240 μM (EC50) |
α3β2α5 360 μM (EC50) |
α3β4 NA μM (EC50) |
Rivanicline hemioxalate (75-125 µmol/kg, s.c., single dose) can cause a decrease in body temperature, respiratory rate, Y-maze activity and auditory startle response, but its potency is significantly lower than that of nicotine in mice physiological test battery model[2].
Rivanicline hemioxalate (2 mg/kg, i.p., single dose) restores the learning ability of mice in impairment of eyeblink conditioning model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Scopolamine (1.3 μmol/kg)-induced passive amnesia model established in male wistar rats (200-220 g)[2]
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Dosage:0.06, 0.6, 6 µmol/kg
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Administration:Subcutaneous Injections (s.c.), 30 min before testing
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Result:Reversed scopolamine-induced amnesia, increasing step-through latency at 0.6 µmol/kg.
No effect at 0.06 or 6 µmol/kg.
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Animal Model:Ibotenic acid lesion radial arm maze model established in male Sprague-Dawley rats (250–270 g) [2]
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Dosage:0, 0.3, 0.6, 0.9, 1.2 µmol/kg
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Administration:Subcutaneous Injections (s.c.), 20 min before testing
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Result:Improved working memory (place task) in lesioned rats.
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Animal Model:Physiological test battery model established in C57BL/6 mice[2]
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Dosage:75, 100 and 125 µmol/kg
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Administration:Subcutaneous Injections (s.c.), single dose
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Result:Was 15-50x less potent than nicotine in reducing body temperature, respiration, and locomotor activity.
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Animal Model:MK-801 (0.02 mg/kg)-induced impairment of eyeblink conditioning model established in C57Bl/6 mice (3-5 months)[4]
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Dosage:2 mg/kg
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Administration:Intraperitoneal injection (i.p.), single dose
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Result:Rescues learning by activating presynaptic nAChRs to enhance glutamate release.
Chemical Information
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Appearance Solid
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Molecular Weight 207.23
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Formel C11H15N2O2
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Color White to off-white
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SMILES
CNCC/C=C/C1=CC=CN=C1.OC(C(O)=O)=O.[0.5]
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Synonyms
RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
α4 nicotinic receptors on GABAergic neurons mediate a cholinergic analgesic circuit in the substantia nigra pars reticulata. [Abstract]2024 Jun;45(6):1160-1174. PMID: 38438581
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (241.28 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 (sealed storage, 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 (sealed storage, 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (12.06 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 (12.06 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Reinheit & Dokumentation
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Data Sheet (282 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)
Verweise
[1]. Bencherif M, et al. RJR-2403: a nicotinic agonist with CNS selectivity I. In vitro characterization. J Pharmacol Exp Ther. 1996 Dec;279(3):1413-21. [Content Brief]
[2]. Lippiello PM, et al. RJR-2403: a nicotinic agonist with CNS selectivity II. In vivo characterization. J Pharmacol Exp Ther. 1996 Dec;279(3):1422-9. [Content Brief]
[3]. Papke RL, et al The activation and inhibition of human nicotinic acetylcholine receptor by RJR-2403 indicate a selectivity for the alpha4beta2 receptor subtype. J Neurochem. 2000 Jul;75(1):204-16. [Content Brief]
[4]. Rodríguez-Moreno A, et al. The nicotinic agonist RJR-2403 compensates the impairment of eyeblink conditioning produced by the noncompetitive NMDA-receptor antagonist MK-801. Neurosci Lett. 2006 Jul 10;402(1-2):102-7. [Content Brief]
[5]. Damaj MI, et al. Antinociceptive and pharmacological effects of metanicotine, a selective nicotinic agonist. J Pharmacol Exp Ther. 1999 Oct;291(1):390-8. [Content Brief]
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 (sealed storage, 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 | 4.8256 mL | 24.1278 mL | 48.2556 mL | 120.6389 mL |
| 5 mM | 0.9651 mL | 4.8256 mL | 9.6511 mL | 24.1278 mL | |
| 10 mM | 0.4826 mL | 2.4128 mL | 4.8256 mL | 12.0639 mL | |
| 15 mM | 0.3217 mL | 1.6085 mL | 3.2170 mL | 8.0426 mL | |
| 20 mM | 0.2413 mL | 1.2064 mL | 2.4128 mL | 6.0319 mL | |
| 25 mM | 0.1930 mL | 0.9651 mL | 1.9302 mL | 4.8256 mL | |
| 30 mM | 0.1609 mL | 0.8043 mL | 1.6085 mL | 4.0213 mL | |
| 40 mM | 0.1206 mL | 0.6032 mL | 1.2064 mL | 3.0160 mL | |
| 50 mM | 0.0965 mL | 0.4826 mL | 0.9651 mL | 2.4128 mL | |
| 60 mM | 0.0804 mL | 0.4021 mL | 0.8043 mL | 2.0106 mL | |
| 80 mM | 0.0603 mL | 0.3016 mL | 0.6032 mL | 1.5080 mL | |
| 100 mM | 0.0483 mL | 0.2413 mL | 0.4826 mL | 1.2064 mL |
Rivanicline hemioxalate Related Classifications
HY-13225B Related Classifications
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