Facinicline (free base) | CAS#677306-35-3 | CAS#677305-02-1 | nicotinic alpha-7 (α7) receptor agonist

Facinicline free base

WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 319747

CAS#: 677306-35-3 (free base)

Description: Facinicline, also known as RG-3487, R-3487 or MEM-3454, is a partial agonist of the nicotinic alpha-7 (α7) receptor that was being co-developed by Roche for the oral treatment of Alzheimer's.

Chemical Structure

Facinicline free base

CAS# 677306-35-3 (free base)

Instruction

Theoretical Analysis

MedKoo Cat#: 319747
Name: Facinicline free base
CAS#: 677306-35-3 (free base)
Chemical Formula: C15H18N4O
Exact Mass: 270.15
Molecular Weight: 270.336
Elemental Analysis: C, 66.64; H, 6.71; N, 20.73; O, 5.92

Price and Availability

Size	Price	Availability	Quantity
1g	USD -1
2g	USD -1
5g	USD -1
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 677306-35-3 (free base) 677305-02-1(HCl)

Synonym: Facinicline; RG-3487; RG 3487; RG3487; R-3487; R 3487; R3487; RO-5313534; RO 5313534; RO5313534; MEM3454; MEM 3454; MEM-3454;

IUPAC/Chemical Name: (S)-N-(quinuclidin-3-yl)-1H-indazole-3-carboxamide

InChi Key: TXCYUSKWBHUVEP-CYBMUJFWSA-N

InChi Code: InChI=1S/C15H18N4O/c20-15(14-11-3-1-2-4-12(11)17-18-14)16-13-9-19-7-5-10(13)6-8-19/h1-4,10,13H,5-9H2,(H,16,20)(H,17,18)/t13-/m1/s1

SMILES Code: C1CN2CCC1[C@@H](C2)NC(=O)C3=NNC4=CC=CC=C43

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Related CAS# 677306-35-3(Facinicline Free Base) 677305-02-1(Facinicline HCl)

Instruction:

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Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 270.34 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Umbricht D, Keefe RS, Murray S, Lowe DA, Porter R, Garibaldi G, Santarelli L. A randomized, placebo-controlled study investigating the nicotinic α7 agonist, RG3487, for cognitive deficits in schizophrenia. Neuropsychopharmacology. 2014 Jun;39(7):1568-77. doi: 10.1038/npp.2014.17. PubMed PMID: 24549101; PubMed Central PMCID: PMC4023143.

2: Wallace TL, Callahan PM, Tehim A, Bertrand D, Tombaugh G, Wang S, Xie W, Rowe WB, Ong V, Graham E, Terry AV Jr, Rodefer JS, Herbert B, Murray M, Porter R, Santarelli L, Lowe DA. 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. doi: 10.1124/jpet.110.171892. PubMed PMID: 20959364.

3: Huang M, Felix AR, Kwon S, Lowe D, Wallace T, Santarelli L, Meltzer HY. The alpha-7 nicotinic receptor partial agonist/5-HT3 antagonist RG3487 enhances cortical and hippocampal dopamine and acetylcholine release. Psychopharmacology (Berl). 2014 May;231(10):2199-210. doi: 10.1007/s00213-013-3373-5. PubMed PMID: 24317442.

4: Kuang S, Zhang P, Dong EZ, Jennings G, Zhao B, Pierce M. Crystal form control and particle size control of RG3487, a nicotinic α7 receptor partial agonist. Int J Pharm. 2016 Jul 11;508(1-2):109-22. doi: 10.1016/j.ijpharm.2016.04.066. PubMed PMID: 27167333.

5: 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. doi: 10.1089/adt.2014.622. PubMed PMID: 25880723.

6: 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. PubMed PMID: 26044974; PubMed Central PMCID: PMC5024727.

7: Pohanka M. Alpha7 nicotinic acetylcholine receptor is a target in pharmacology and toxicology. Int J Mol Sci. 2012;13(2):2219-38. doi: 10.3390/ijms13022219. Review. PubMed PMID: 22408449; PubMed Central PMCID: PMC3292018.

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