WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H319747
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.
Hodoodo Cat#: H319747
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
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)
Biological target: | |
In vitro activity: | |
In vivo activity: |
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: |
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.