カタログ番号 T12738
別名:
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, CAS N/A
| パッケージサイズ |
在庫状況 |
単価(税別) |
| 500 mg |
約10-14 週間 |
￥ 407,500 |
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生物学的特性に関する説明
化学的特性
保存条件
& 溶解度情報
| 説明 |
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. |
| 別名 |
RJR-2403 hemioxalate, (E)-Metanicotine hemioxalate
|
| 分子量 |
207.23
|
| 分子式 |
C12H16N2O4 |
保存条件
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度情報
DMSO: 50 mg/mL (241.28 mM),
Sonication is recommended.
参考文献
投与量変換
You can also refer to dose conversion for different animals.
詳細
In vivo投与量計算 (透明溶液)
ステップ1: 以下の情報を入力してください
溶媒の組成を入力してください
計算器
モル濃度計算機
希釈計算機
再構成計算
分子量計算機
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技術サポート
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
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
inhibitor
inhibit
