2-Hydroxysaclofen
Based on 1 Customer Validation
2-Hydroxysaclofen is a potent γ-amino-butyric-acid-B (GABAB) receptor antagonist. 2-Hydroxysaclofen can abolish nicotine-induced hypolocomotor effects and increases the antinociceptive effects. 2-Hydroxysaclofen can stimulate luteinizing hormone (LH) secretion in female rats.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 117354-64-0
- Formula: C9H12ClNO4S
- Molecular Weight:265.71
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Storage:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
GABAB receptor[1]
2-Hydroxysaclofen (0.3-3 mg/kg; IP; single dosage) reduces the effects of Baclofen (a GABA receptor agonist) on d-amphetamine-induced discriminative cue[2].
2-Hydroxysaclofen (0-100 μg/2 μl; ICV; single dosage) produces a rapid elevation in the serum LH concentration in the estrogen-primed ovariectomized rat[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Swiss Webster mice (22-24 g; treated with 3 mg/kg nicotine)[1]
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Dosage:0.25, 0.5 and 1 mg/kg
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Administration:IP; single dosage; after 10 or 45 min of nicotine administration
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Result:Abolished nicotine hypolocomotor effects at 1 mg/kg, and increased the antinociceptive effects of nicotine at 1 mg/kg.
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Animal Model:Male Wistar rats[2]
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Dosage:0.3, 1 and 3 mg/kg
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Administration:IP; single dosage
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Result:Reduced the effects of Baclofen on d-amphetamine-induced discriminative cue.
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Animal Model:Female Wistar rats (8 weeks)[3]
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Dosage:0, 20, 50 or 100 μg/2 μL
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Administration:ICV; single dosage
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Result:Produced a rapid elevation in the serum LH concentration in the estrogen-primed ovariectomized rat with a dose-dependent manner, and the peak LH values were observed 10 min after the injection.
The effect was dose-dependent, as 0 or 20 μg of the antagonist was ineffective while a pronounced effect was observed after the injection of 50 or 100 μg.
Chemical Information
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CAS No. 117354-64-0
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Appearance Solid
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Molecular Weight 265.71
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Formula C9H12ClNO4S
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Color White to off-white
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SMILES
O=S(CC(O)(CN)C1=CC=C(Cl)C=C1)(O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
H2O : 50 mg/mL (188.18 mM; ultrasonic and adjust pH to 11 with 1 M NaOH)
1M NaOH : 26.57 mg/mL (100.00 mM; Need ultrasonic and warming)
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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (279 KB)
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SDS (417 KB)
- English - EN (417 KB)
- Français - FR (417 KB)
- Deutsch - DE (417 KB)
- Norwegian - NO (417 KB)
- Español - ES (417 KB)
- Swedish - SV (417 KB)
- Italian - IT (417 KB)
- Korean - KR (417 KB)
- Portuguese - PT (417 KB)
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Handling Instructions (2659 KB)
References
[1]. Varani AP, et al. Baclofen and 2-hydroxysaclofen modify acute hypolocomotive and antinociceptive effects of nicotine. Eur J Pharmacol. 2014 Sep 5;738:200-5. [Content Brief]
[2]. Miranda F, et al. The GABA-B antagonist 2-hydroxysaclofen reverses the effects of baclofen on the discriminative stimulus effects of D-amphetamine in the conditioned taste aversion procedure. Pharmacol Biochem Behav. 2009 Jul;93(1):25-30. [Content Brief]
[3]. Akema T, et al. 2-Hydroxysaclofen, a potent GABAB receptor antagonist, stimulates luteinizing hormone secretion in female rats. Brain Res. 1991 Apr 12;546(1):143-5. [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 (protect from light, stored under nitrogen). 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 |
|---|---|---|---|---|---|
| 1M NaOH / H2O | 1 mM | 3.7635 mL | 18.8175 mL | 37.6350 mL | 94.0875 mL |
| 5 mM | 0.7527 mL | 3.7635 mL | 7.5270 mL | 18.8175 mL | |
| 10 mM | 0.3764 mL | 1.8818 mL | 3.7635 mL | 9.4088 mL | |
| 15 mM | 0.2509 mL | 1.2545 mL | 2.5090 mL | 6.2725 mL | |
| 20 mM | 0.1882 mL | 0.9409 mL | 1.8818 mL | 4.7044 mL | |
| 25 mM | 0.1505 mL | 0.7527 mL | 1.5054 mL | 3.7635 mL | |
| 30 mM | 0.1255 mL | 0.6273 mL | 1.2545 mL | 3.1363 mL | |
| 40 mM | 0.0941 mL | 0.4704 mL | 0.9409 mL | 2.3522 mL | |
| 50 mM | 0.0753 mL | 0.3764 mL | 0.7527 mL | 1.8818 mL | |
| 60 mM | 0.0627 mL | 0.3136 mL | 0.6273 mL | 1.5681 mL | |
| 80 mM | 0.0470 mL | 0.2352 mL | 0.4704 mL | 1.1761 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.
2-Hydroxysaclofen Related Classifications
HY-100812 Related Classifications
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