| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Rivanicline hemioxalate primarily targets the alpha4beta2 subtype of neuronal nicotinic acetylcholine receptors (nAChRs). It exhibits high affinity for this receptor, with a Ki value of 26 nM in rat brain cortex. The compound shows more than 1,000-fold selectivity for alpha4beta2 over alpha7 receptors (Ki=3.6 microM), making it a highly selective tool for studying this receptor subtype. It does not significantly activate muscle-type nAChRs or muscarinic receptors.
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| ln Vitro |
In vitro, Rivanicline hemioxalate activates rat thalamic synaptosomes with an EC50 of 732 nM, comparable to nicotine. It displays less than one-tenth the potency of nicotine in inducing ileum contraction, with substantially lower efficacy. Chronic exposure to 10 microM leads to up-regulation of high-affinity nAChRs in M10 cells, mimicking effects observed with nicotine.
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| ln Vivo |
In vivo, Rivanicline significantly reversed scopolamine-induced amnesia and improved both working and reference memory in a rat model. It is 15 to 30 times less potent than nicotine in affecting body temperature, respiration, and other physiological responses, demonstrating greatly reduced cardiovascular effects. Its potency is approximately five times lower than nicotine in tail-flick tests following subcutaneous administration.
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| Enzyme Assay |
A cell-free receptor binding assay is performed using membranes from rat brain cortex or cells expressing recombinant alpha4beta2 nAChRs. Membranes (10-20 ug protein) are incubated with a radiolabeled ligand (e.g., [3H]cytisine or [3H]epibatidine, 0.5-2 nM) and increasing concentrations (0.01-10,000 nM) of Rivanicline in binding buffer. Nonspecific binding is determined with 10 uM nicotine. Bound radioligand is separated by filtration through GF/B filters and counted. Ki values are calculated from competition curves.
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| Cell Assay |
For a functional cell-based assay, SH-EP1 cells stably expressing human alpha4beta2 nAChRs are seeded in 96-well plates. Cells are loaded with a calcium-sensitive dye (e.g., Fluo-4 AM, 4 uM) for 30-60 min. Rivanicline hemioxalate is added at varying concentrations (0.1-10,000 nM). The increase in intracellular calcium is measured using a FlexStation or FLIPR (ex/em = 485/535 nm). The EC50 for receptor activation is calculated from the dose-response curve (reference EC50 ~732 nM).
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| Animal Protocol |
Rivanicline hemioxalate can be studied in rat models of memory impairment. Male Sprague-Dawley rats (200-250 g, n=8-12 per group) are injected with scopolamine (1 mg/kg, i.p.) to induce amnesia. Rivanicline (0.1-1 mg/kg, i.p.) is administered 15-30 min before behavioral testing. Passive avoidance retention (step-through latency) and working memory (radial arm maze) are assessed. The compound significantly reverses scopolamine-induced memory deficits.
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| ADME/Pharmacokinetics |
Rivanicline hemioxalate has a molecular weight of 207.23 and the molecular formula C12H16N2O4. The powder should be stored at -20degC for up to 3 years. In solvent, it is stable for 1 year at -80degC. The compound is soluble in DMSO (50 mg/mL). Specific PK parameters (t½, Cmax, AUC) have not been fully reported. Rivanicline is 15-30 times less potent than nicotine in affecting body temperature and respiration.
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| Toxicity/Toxicokinetics |
Rivanicline hemioxalate is generally well-tolerated at the doses used in animal studies (0.1-1 mg/kg). It shows greatly reduced cardiovascular effects compared to nicotine, indicating a favorable safety profile. However, formal toxicology studies have not been published. As a nicotinic agonist, potential side effects include mild autonomic responses at higher doses. Standard safety precautions should be followed.
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| References |
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| Additional Infomation |
Rivanicline hemioxalate is a research-grade compound and is not approved for clinical use. It is a highly selective alpha4beta2 nicotinic receptor agonist that has been studied for its cognitive-enhancing properties. This product is for research use only and not for human therapeutic applications. The hemioxalate salt enhances solubility.
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| Molecular Formula |
C11H15N2O2
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| Molecular Weight |
207.23
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| Related CAS # |
Rivanicline oxalate;220662-95-3;Rivanicline;15585-43-0
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| Appearance |
White to off-white solid powder
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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, 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 :~50 mg/mL (~241.28 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.06 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (12.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8256 mL | 24.1278 mL | 48.2556 mL | |
| 5 mM | 0.9651 mL | 4.8256 mL | 9.6511 mL | |
| 10 mM | 0.4826 mL | 2.4128 mL | 4.8256 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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