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Facinicline hydrochloride

Catalog No. T28531 CAS 677305-02-1

Synonyms: RG3487

Facinicline hydrochloride (RG3487) is both a novel nicotinic alpha-7 receptor (alpha7nAChR) partial agonist (Ki = 6 nM) and an antagonist of 5-HT3(Ki = 1.2 nM). Facinicline hydrochloride improves cognition and sensorimotor gating in rodents.

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Facinicline hydrochloride Chemical Structure

Facinicline hydrochloride, CAS 677305-02-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 97.00
5 mg	In stock	$ 247.00
10 mg	In stock	$ 413.00
25 mg	In stock	$ 692.00
50 mg	In stock	$ 985.00
100 mg	In stock	$ 1,330.00
1 mL * 10 mM (in DMSO)	In stock	$ 272.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Facinicline hydrochloride (RG3487) is both a novel nicotinic alpha-7 receptor (alpha7nAChR) partial agonist (Ki = 6 nM) and an antagonist of 5-HT3(Ki = 1.2 nM). Facinicline hydrochloride improves cognition and sensorimotor gating in rodents.
Targets&IC50	α7 nAChR:6 nM (Ki), 5-HT3 receptor:1.2 nM (Ki)
In vitro	Facinicline hydrochloride exhibits antagonist properties at the serotonin 3 receptor in oocytes(IC50 = 2.8 μM) and N1E-115 cells(IC50 = 32.7 μM)[2].Facinicline hydrochloride activates human α7 nAChRs in oocytes(EC50 = 0.8 μM) and QM7 cells(EC50 = 7.7 μM)[2].
In vivo	In Male Sprague-Dawley rats, Facinicline hydrochloride (0.1–10 mg/kg p.o.) selectively enhances object recognition memory[1]. Facinicline hydrochloride improves object recognition memory in rats after acute(1.0 mg/kg p.o.) or repeated (10 day) administration at brain and plasma concentrations in the low-nanomolar range[2].

Synonyms	RG3487
Molecular Weight	306.79
Formula	C15H19ClN4O
CAS No.	677305-02-1

Storage

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

Solubility Information

H2O: 100 mg/mL (325.96 mM)

DMSO: 125 mg/mL (407.44 mM)

References and Literature

1. Boess F, et al. Use of early phenotypic in vivo markers to assess human relevance of an unusual rodent non-genotoxic carcinogen in vitro. Toxicology. 2017 Mar 15;379:48-61. 2. Tanya L Wallace, et al. RG3487, a Novel Nicotinic α7 Receptor Partial Agonist, Improves Cognition and Sensorimotor Gating in Rodents. J Pharmacol Exp Ther. 2011 Jan;336(1):242-53. 3. Hashimoto K. Targeting of α7 Nicotinic Acetylcholine Receptors in the Treatment of Schizophrenia and the Use of Auditory Sensory Gating as a Translational Biomarker. Curr Pharm Des. 2015;21(26):3797-806. Review. 4. Hao Y, Tang J, Wang K. Development of Automated Patch Clamp Assay for Evaluation of α7 Nicotinic Acetylcholine Receptor Agonists in Automated QPatch-16. Assay Drug Dev Technol. 2015 Apr;13(3):174-84.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library GPCR Compound Library Bioactive Compound Library Neuronal Signaling Compound Library Anti-Cancer Compound Library Neurotransmitter Receptor Compound Library Serotonin Receptor-Targeted Compound Library Bioactive Compounds Library Max Orally Active Compound Library

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Keywords

Facinicline hydrochloride 677305-02-1 GPCR/G Protein Neuroscience AChR 5-HT Receptor Inhibitor nAChR serotonin 3 receptor Facinicline Hydrochloride RG3487 Nicotinic acetylcholine receptors Serotonin Receptor RG-3487 inhibit recognition 5-hydroxytryptamine Receptor RG 3487 Facinicline receptor memory nicotinic inhibitor

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