Saclofen
Based on 5 publication(s) in Google Scholar
Saclofen is an orally active and a competitive GABAB receptor antagonist with an IC50 of 7.8 μM. Saclofen has weak antagonistic effects on GABAB1b and GABAB2 heterodimeric recombinant receptors. Saclofen inhibits the binding of Baclofen (HY-B0007) to rat cerebellar membranes and blocks Baclofen-induced circadian phase shifts, and exhibits anti-inflammatory and analgesic effects in rats.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 99.97%
- CAS 番号: 125464-42-8
- 分子式: C9H12ClNO3S
- 分子量:249.72
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
Saclofen (300 μM, 0-24 h) inhibits the phase changes in the circadian rhythm caused by Baclofen in brain slices of the rat suprachiasmatic nucleus (SCN) [1].
Saclofen (0.1 μM-1 mM, 10 s) suppresses the increase in CHO intracellular calcium induced by GABA at high concentrations[2].
Saclofen inhibits the binding of Baclofen to rat cerebellar membranes with an IC50 of 7.8 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Saclofen (1mg/mL, i.p., single dose) has analgesic effects in a rat pain model induced by acetic acid[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Wistar rats induced by lipopolysaccharide(LPS)[3]
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Dosage:50 μg/10 μL/rat
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Administration:i.c.
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Result:Eliminated the hypotensive effect of lipopolysaccharide (LPS), restored mean arterial pressure (MAP), and reduced the increase of TNF-α and IL-6 induced by LPS.
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Animal Model:Acetic acid -induced visceral pain by in rat[4]
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Dosage:1 mg/kg, single dose
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Administration:Intraperitoneal injection (i.p.)
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Result:Could prevent pain caused by the GABAB receptor agonist baclofen.
化学情報
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CAS 番号 125464-42-8
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性状 Solid
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分子量 249.72
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分子式 C9H12ClNO3S
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Color White to off-white
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SMILES
O=S(CC(CN)C1=CC=C(Cl)C=C1)(O)=O
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別名
サクロフェン
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Commun
2025 May 15;16(1):4521. PMID: 40374633 -
J Adv Res
Gut microbial GABAergic signaling improves stress-associated innate immunity to respiratory viral infection. [Abstract]2024 Jun:60:41-56. PMID: 37353002 -
Toxicol Sci
Perfluorooctanesulfonic acid (PFOS) antagonizes gamma-aminobutyric acid (GABA) receptors in larval zebrafish and mammalian models. [Abstract]2025 Jul 23:kfaf101. PMID: 40700607 -
Biochem Biophys Res Commun
2023 Nov 12:681:80-89. PMID: 37774573 -
溶剤 & 溶解度
H2O : 10 mg/mL (40.04 mM; Need ultrasonic)
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. 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. 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)
純度とドキュメンテーション
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データシート (279 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. K R Biggs, et al. GABAB receptor stimulation phase-shifts the mammalian circadian clock in vitro. Brain Res. 1998 Oct 5;807(1-2):250-4. [Content Brief]
[2]. M D Wood, et al. The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen. Br J Pharmacol. 2000 Nov;131(6):1050-4. [Content Brief]
[3]. Sallam MY, et al. Central GABAA receptors are involved in inflammatory and cardiovascular consequences of endotoxemia in conscious rats. Naunyn Schmiedebergs Arch Pharmacol. 2016 Mar;389(3):279-88. [Content Brief]
[5]. C A Drew, et al. Inhibition of baclofen binding to rat cerebellar membranes by phaclofen, saclofen, 3-aminopropylphosphonic acid and related GABAB receptor antagonists. Neurosci Lett. 1990 May 18;113(1):107-10. [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. 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 | 4.0045 mL | 20.0224 mL | 40.0449 mL | 100.1121 mL |
| 5 mM | 0.8009 mL | 4.0045 mL | 8.0090 mL | 20.0224 mL | |
| 10 mM | 0.4004 mL | 2.0022 mL | 4.0045 mL | 10.0112 mL | |
| 15 mM | 0.2670 mL | 1.3348 mL | 2.6697 mL | 6.6741 mL | |
| 20 mM | 0.2002 mL | 1.0011 mL | 2.0022 mL | 5.0056 mL | |
| 25 mM | 0.1602 mL | 0.8009 mL | 1.6018 mL | 4.0045 mL | |
| 30 mM | 0.1335 mL | 0.6674 mL | 1.3348 mL | 3.3371 mL | |
| 40 mM | 0.1001 mL | 0.5006 mL | 1.0011 mL | 2.5028 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.
Saclofen 関連分類
HY-100813 関連分類
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