2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. 2-Hydroxysaclofen

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.

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2-Hydroxysaclofen Chemical Structure

2-Hydroxysaclofen Chemical Structure

CAS No. : 117354-64-0

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2-Hydroxysaclofen Related Antibodies

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Description

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[1][2][3].

IC50 & Target

GABAB receptor[1]
In Vivo

2-Hydroxysaclofen (0.25-1 mg/kg; IP; single dosage) abolishes nicotine hypolocomotor effects and increases the antinociceptive effects of nicotine[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.

Animal Model: Male Swiss Webster mice (22-24 g; treated with 3 mg/kg nicotine)[1]
Dosage: 0.25, 0.5 and 1 mg/kg
Administration: IP; single dosage; after 10 or 45 min of nicotine administration
Result: Abolished nicotine hypolocomotor effects at 1 mg/kg, and increased the antinociceptive effects of nicotine at 1 mg/kg.
Animal Model: Male Wistar rats[2]
Dosage: 0.3, 1 and 3 mg/kg
Administration: IP; single dosage
Result: Reduced the effects of Baclofen on d-amphetamine-induced discriminative cue.
Animal Model: Female Wistar rats (8 weeks)[3]
Dosage: 0, 20, 50 or 100 μg/2 μL
Administration: ICV; single dosage
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.
Molecular Weight

265.71

Formula

C9H12ClNO4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(CC(O)(CN)C1=CC=C(Cl)C=C1)(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7635 mL 18.8175 mL 37.6350 mL
5 mM 0.7527 mL 3.7635 mL 7.5270 mL
View the 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.

* 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.

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Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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.

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2-Hydroxysaclofen Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

2-Hydroxysaclofen117354-64-0GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorNicotinehypolocomotorantinociceptiveluteinizing hormoneInhibitorinhibitorinhibit

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