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Rivanicline hemioxalate

Catalog No. T12738 CAS T12738

Synonyms: RJR-2403 hemioxalate, (E)-Metanicotine hemioxalate

Rivanicline hemioxalate, also known as RJR-2403 hemioxalate or (E)-Metanicotine hemioxalate, is a chemical compound acting as a neuronal nicotinic receptor agonist with pronounced selectivity for the α4β2 receptor subtype, showing over 1,000-fold greater selectivity for this subtype (Ki=26 nM) compared to α7 receptors (Ki=3.6 μM). Its in vitro studies demonstrate no significant activation of nAChRs in PC12 cells, muscle type nAChRs, or muscarinic receptors at concentrations up to 1 mM. Furthermore, Rivanicline displayed less than one-tenth the potency of nicotine in inducing ileum contraction, with substantially lower efficacy, and failed to antagonize nicotine-induced stimulation of muscle or ganglionic nAChR functions, with an IC50 value greater than 1 mM. Chronic exposure to Rivanicline at 10 microM led to up-regulation of high-affinity nAChRs in M10 cells, mimicking effects observed with nicotine. In vivo studies revealed that Rivanicline significantly reversed scopolamine-induced amnesia and improved working and reference memory in a rat model, while being 15 to 30 times less potent than nicotine in affecting body temperature, respiration, and other physiological responses. Metanicitone’s potency was approximately five times lower than nicotine in tail-flick tests following subcutaneous administration, yet slightly more potent upon central administration.

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Rivanicline hemioxalate Chemical Structure

Rivanicline hemioxalate, CAS T12738

Pack Size	Availability	Price/USD	Quantity
500 mg	10-14 weeks	$ 1,774.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description

Synonyms	RJR-2403 hemioxalate, (E)-Metanicotine hemioxalate
Molecular Weight	207.23
Formula	C12H16N2O4
CAS No.	T12738

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (241.28 mM), Sonication is recommended.

References and Literature

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. 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. 3. Damaj MI, et al. Antinociceptive and pharmacological effects of metanicotine, a selective nicotinic agonist. J Pharmacol Exp Ther. 1999 Oct;291(1):390-8.

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Rivanicline hemioxalate T12738 Others RJR2403 Hemioxalate Metanicotine Hemioxalate Metanicotine RJR-2403 RJR-2403 Hemioxalate RJR2403 RJR 2403 RJR-2403 hemioxalate Rivanicline Hemioxalate RJR 2403 Hemioxalate Rivanicline (E)-Metanicotine hemioxalate inhibitor inhibit

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