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2-Hydroxysaclofen is a potent γ-amino-butyric-acid-B receptor antagonist that effectively abolishes nicotine-induced hypolocomotor effects, enhances antinociceptive responses, and stimulates luteinizing hormone secretion in female rats, making it a valuable pharmacological probe for investigating GABAB receptor–mediated neuroendocrine regulation and behavioral pharmacology.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $89 | - | In Stock | |
| 5 mg | $219 | - | In Stock | |
| 10 mg | $326 | - | In Stock | |
| 25 mg | $546 | - | In Stock | |
| 50 mg | $778 | - | In Stock | |
| 100 mg | $1,060 | - | In Stock |
| Description | 2-Hydroxysaclofen is a potent γ-amino-butyric-acid-B receptor antagonist that effectively abolishes nicotine-induced hypolocomotor effects, enhances antinociceptive responses, and stimulates luteinizing hormone secretion in female rats, making it a valuable pharmacological probe for investigating GABAB receptor–mediated neuroendocrine regulation and behavioral pharmacology. |
| In vivo | In male Swiss Webster mice, intraperitoneal (IP) administration of 2-Hydroxysaclofen (0.25-1 mg/kg) modulates the acute effects of nicotine. At a dose of 1 mg/kg, it abolishes nicotine-induced hypolocomotion while enhancing its antinociceptive effects. In male Wistar rats, IP administration (0.3-3 mg/kg) antagonizes the ability of Baclofen to alter the discriminative stimulus effects of d-amphetamine. Furthermore, in estrogen-primed ovariectomized female rats, intracerebroventricular (ICV) injection (50-100 ug/mL) leads to an elevation in serum Luteinizing Hormone (LH) concentrations, with peak levels observed 10 minutes post-injection [1][2][3]. |
| Molecular Weight | 265.71 |
| Formula | C9H12ClNO4S |
| Cas No. | 117354-64-0 |
| Smiles | O=S(=O)(O)CC(O)(C1=CC=C(Cl)C=C1)CN |
| Relative Density. | 1.551 g/cm3 |
| Storage | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | 1M NaOH: 25 mg/mL (94.09 mM), Sonication is recommended. H2O: 40 mg/mL (150.54 mM), when pH is adjusted to 11 with 1 M NaOH. Sonication is recommmended. 1eq. NaOH: 100 mM, Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
1M NaOH/1eq. NaOH/H2O
1eq. NaOH/H2O
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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