| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
SIB-1553A HCl targets nicotinic acetylcholine receptors (nAChRs) with selectivity for the β4 subunit-containing receptors.
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| 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).
In vitro, SIB-1553A HCl acts as a selective agonist at β4 subunit-containing nAChRs. It stimulates the release of acetylcholine and other neurotransmitters relevant for cognitive processes. |
| ln Vivo |
SIB-1553A (1-40 mg/kg; subcutaneous injection) raises acetylcholine levels in a dose-dependent manner [3].
In vivo, SIB-1553A HCl improves both attention and memory components of a spatial working memory task in chronic low-dose MPTP-treated monkeys. It has shown potential as a cognitive enhancer in models of Alzheimer's disease and cognitive impairment. |
| Enzyme Assay |
In vitro receptor binding assays for SIB-1553A HCl are performed using membrane preparations from cells expressing different nAChR subunit combinations. Radioligand binding studies with [³H]epibatidine or other nAChR ligands are used to determine the compound's affinity and selectivity for β4-containing receptors compared to other nAChR subtypes (e.g., α7, α4β2).
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| Cell Assay |
In vitro cellular assays for SIB-1553A HCl involve measuring its agonistic activity at nAChRs. Cells expressing the receptor are treated with the compound, and the influx of calcium or other ions is measured using fluorescent dyes (e.g., Fluo-4). The compound's ability to stimulate neurotransmitter release can be assessed in synaptosome preparations.
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| 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. In vivo animal experiments for SIB-1553A HCl are conducted in primate models of cognitive impairment, such as MPTP-treated monkeys, as well as in rodent models of Alzheimer's disease. The compound is administered orally, and cognitive performance is assessed using tasks like the delayed matching-to-sample (DMTS) or Morris water maze. Neurochemical effects are measured by microdialysis. |
| ADME/Pharmacokinetics |
As an orally available compound, SIB-1553A HCl is expected to have good oral bioavailability and brain penetration. Its PK properties have been characterized in preclinical species, supporting its use in cognitive research.
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| Toxicity/Toxicokinetics |
Toxicological data for SIB-1553A HCl are not detailed in publicly available sources. As a research compound, its safety profile has been evaluated in animal models. No significant toxicity has been reported in the available literature.
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| References |
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| Additional Infomation |
SIB-1553A HCl is a research compound and a selective nicotinic acetylcholine receptor agonist. It is studied for its potential in treating cognitive disorders, including Alzheimer's disease. It is not an approved drug and is used as a tool to study the role of nAChRs in cognition.
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| Molecular Formula |
C13H20CLNOS
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|---|---|
| Molecular Weight |
273.82
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| Exact Mass |
273.095
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| CAS # |
191611-89-9
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| PubChem CID |
9881989
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
17
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| Complexity |
204
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CCCC1CCSC2=CC=C(C=C2)O.Cl
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| InChi Key |
RJSVKPQKXSMZMT-UHFFFAOYSA-N
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| 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
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| Chemical Name |
4-[2-(1-methylpyrrolidin-2-yl)ethylsulfanyl]phenol;hydrochloride
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| Synonyms |
SIB-1553A; SIB 1553A; SIB1553A
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
H2O : ≥ 27.38 mg/mL (~99.99 mM)
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| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
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.
(2) Be sure to add the solvent(s) in order.
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