SIB-1553A
Based on 1 Customer Validation
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.0%
- CAS 番号: 191611-89-9
- 分子式: C13H20ClNOS
- 分子量:273.82
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
生物活性
SIB-1553A displaces the binding of [H]nicotine (NIC) to the rat brain nAChRs with an IC50 value of 110 nM[1].
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[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (200-250 g)[3]
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Dosage:1, 2, 4, 10, 20 and 40 mg/kg
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Administration:s.c.
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Result:Induced hippocampal ACh release.
化学情報
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CAS 番号 191611-89-9
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性状 Solid
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分子量 273.82
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分子式 C13H20ClNOS
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Color White to off-white
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SMILES
OC(C=C1)=CC=C1SCCC2N(CCC2)C.[H]Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
H2O : ≥ 100 mg/mL (365.20 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (365.20 mM); Clear solution; Need ultrasonic
純度とドキュメンテーション
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データシート (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. 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. [Content Brief]
[2]. 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. [Content Brief]
[3]. 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 3.6520 mL | 18.2602 mL | 36.5203 mL | 91.3009 mL |
| 5 mM | 0.7304 mL | 3.6520 mL | 7.3041 mL | 18.2602 mL | |
| 10 mM | 0.3652 mL | 1.8260 mL | 3.6520 mL | 9.1301 mL | |
| 15 mM | 0.2435 mL | 1.2173 mL | 2.4347 mL | 6.0867 mL | |
| 20 mM | 0.1826 mL | 0.9130 mL | 1.8260 mL | 4.5650 mL | |
| 25 mM | 0.1461 mL | 0.7304 mL | 1.4608 mL | 3.6520 mL | |
| 30 mM | 0.1217 mL | 0.6087 mL | 1.2173 mL | 3.0434 mL | |
| 40 mM | 0.0913 mL | 0.4565 mL | 0.9130 mL | 2.2825 mL | |
| 50 mM | 0.0730 mL | 0.3652 mL | 0.7304 mL | 1.8260 mL | |
| 60 mM | 0.0609 mL | 0.3043 mL | 0.6087 mL | 1.5217 mL | |
| 80 mM | 0.0457 mL | 0.2283 mL | 0.4565 mL | 1.1413 mL | |
| 100 mM | 0.0365 mL | 0.1826 mL | 0.3652 mL | 0.9130 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.