Description
SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.
Product information
CAS Number: 191611-89-9
Molecular Weight: 273.82
Formula: C13H20ClNOS
Chemical Name: 4-{[2-(1-methylpyrrolidin-2-yl)ethyl]sulfanyl}phenol; chlorohydrogen
Smiles: Cl.CN1CCCC1CCSC1C=CC(O)=CC=1
InChiKey: RJSVKPQKXSMZMT-UHFFFAOYSA-N
InChi: InChI=1S/C13H19NOS.ClH/c1-14-9-2-3-11(14)8-10-16-13-6-4-12(15)5-7-13;/h4-7,11,15H,2-3,8-10H2,1H3;1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
SIB-1553A displaces the binding of [H]nicotine (NIC) to the rat brain nAChRs with an IC50 value of 110 nM. In calcium flux assays, SIB-1553A (0.1-5 μM), shows a greater selectivity for beta4-subunit containing recombinant hnAChRs (alpha2beta4, alpha3beta4 and alpha4beta4) vs. beta2-subunit containing nAChRs (alpha4beta2 and alpha3beta2) both in terms of efficacy and potency.
In Vivo:
SIB-1553A (1-40 mg/kg; s.c.) produces dose-dependent increases in ACh levels.
References:
- Vernier JM, et al. 4-[[2-(1-Methyl-2-pyrrolidinyl)ethyl]thio]phenol hydrochloride (SIB-1553A): a novel cognitive enhancer with selectivity for neuronal nicotinic acetylcholine receptors. J Med Chem. 1999 May 20;42(10):1684-6.
- Rao TS, et al. In vitro pharmacological characterization of (+/-)-4-[2-(1-methyl-2-pyrrolidinyl)ethyl]thio]phenol hydrochloride (SIB-1553A), a nicotinic acetylcholine receptor ligand. Brain Res. 2003 Aug 15;981(1-2):85-98.
- Rao TS, et al. In vivo pharmacological characterization of (+/-)-4-[2-(1-methyl-2-pyrrolidinyl)ethyl]thiophenol hydrochloride (SIB-1553A), a novel cholinergic ligand: microdialysis studies. Brain Res. 2003 Oct 3;986(1-2):71-81.
Products are for research use only. Not for human use.
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