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Epiboxidine hydrochloride

Catalog No.GC70809 Copy One-Click Copy Product Info

Epiboxidine hydrochloride est un agoniste neuronal puissant et sélectif du nachr avec un Kis de 0,46 nm chez le rat et de 1,2 nm chez l'humain pour l'alpha - 4β2 nachr.

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Epiboxidine hydrochloride Chemical Structure

Cas No.: 862909-67-9

Taille Prix Stock Qté
1 mg
212,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.



Description of Epiboxidine hydrochloride

Epiboxidine hydrochloride is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine hydrochloride is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418.

Epiboxidine hydrochloride has affinity and functional at central neuronal α4β2 receptors, with Kis of 0.46 and 1.2 in rat and humen[1].
Epiboxidine hydrochloride has activity at ganglionic-type α3β4*-nicotinic receptors of PC12 cells, with a Ki of 19[1].
Epiboxidine hydrochloride is much less toxic than Epibatidine[1].
Epiboxidine hydrochloride stimulates sodium-22 influx in PC12 and TE671 cells, with EC50s of 0.18 and 2.6 μM[2].

Epiboxidine hydrochloride (20 μg/kg; ip; once) treatment shows marked analgetic activity in mice[1].
Epiboxidine hydrochloride (50 and 100 mg/kg; intraperitoneal injected; once) causes marked antinociception as measured in the hot-plate assay[2].
Epiboxidine hydrochloride inhibits [3H]nicotine binding in rat cerebral cortical membranes, with a Ki of 0.6 nM[2].

References:
[1]. Fitch RW, et al. Homoepiboxidines: further potent agonists for nicotinic receptors. Bioorg Med Chem. 2004;12(1):179-190.
[2]. Badio B, et al. Synthesis and nicotinic activity of epiboxidine: an isoxazole analogue of epibatidine. Eur J Pharmacol. 1997;321(2):189-194.

Chemical Properties of Epiboxidine hydrochloride

Cas No. 862909-67-9 SDF
Formula C10H15ClN2O M.Wt 214.69
Solubility Storage -20°C, sealed storage, away from moisture
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Epiboxidine hydrochloride

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1 mg 5 mg 10 mg
1 mM 4.6579 mL 23.2894 mL 46.5788 mL
5 mM 931.6 μL 4.6579 mL 9.3158 mL
10 mM 465.8 μL 2.3289 mL 4.6579 mL
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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