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SIB-1553A HCl

Alias: SIB-1553A; SIB 1553A; SIB1553A
Cat No.:V14745 Purity: ≥98%
SIB-1553A is an orally bioavailable nicotinic acetylcholine receptor (nAChRs) agonist selective for the β4 subunit containing nAChRs.
SIB-1553A HCl
SIB-1553A HCl Chemical Structure CAS No.: 191611-89-9
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
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Product Description
SIB-1553A is an orally bioavailable nicotinic acetylcholine receptor (nAChRs) agonist selective for the β4 subunit containing nAChRs. SIB-1553A is also a selective ligand for neuronal nAChR ligands. SIB-1553A is a cognitive enhancer with potential research potential for studying symptoms of Alzheimer's disease (AD) and other cognitive disorders.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
SIB-1553A, which has an IC50 value of 110 nM, substitutes [3H]nicotine (NIC) binding to rat brain nAChR[1]. The β4 subunits (α2β4, α3β4, and α4β4) carrying recombinant hnAChR (α2β4, α3β4, and α4β4) are more selectively bound by SIB-1553A (0.1-5 μM) in a calcium flow experiment than by the β4 subunits containing nAChR (α4β2 and α3β2). potency [2] and the β2 subunits (α4β2 and α3β2).
ln Vivo
SIB-1553A (1-40 mg/kg; subcutaneous injection) raises acetylcholine levels in a dose-dependent manner [3].
Animal Protocol
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (200-250 g) [3]
Doses: 1, 2, 4, 10, 20 and 40 mg/kg
Route of Administration: subcutaneous injection
Experimental Results: Induced hippocampal acetylcholine release.
References

[1]. 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.

[2]. 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.

[3]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C13H20CLNOS
Molecular Weight
273.82
Exact Mass
273.095
CAS #
191611-89-9
PubChem CID
9881989
Appearance
White to off-white solid powder
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
4
Heavy Atom Count
17
Complexity
204
Defined Atom Stereocenter Count
0
InChi Key
RJSVKPQKXSMZMT-UHFFFAOYSA-N
InChi Code
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
Chemical Name
4-[2-(1-methylpyrrolidin-2-yl)ethylsulfanyl]phenol;hydrochloride
Synonyms
SIB-1553A; SIB 1553A; SIB1553A
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
H2O : ≥ 27.38 mg/mL (~99.99 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 100 mg/mL (365.20 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.6520 mL 18.2602 mL 36.5203 mL
5 mM 0.7304 mL 3.6520 mL 7.3041 mL
10 mM 0.3652 mL 1.8260 mL 3.6520 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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