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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $68 | In Stock | |
2 mg | $95 | In Stock | |
5 mg | $147 | In Stock | |
10 mg | $247 | In Stock | |
25 mg | $418 | In Stock | |
50 mg | $596 | In Stock | |
100 mg | $863 | In Stock | |
1 mL x 10 mM (in DMSO) | $133 | In Stock |
Description | GPI-1046 is an immunophilin ligand without antibiotic action and attenuates ethanol intake in part through the upregulation of glutamate transporter 1 (GLT1) in PFC and NAc-core. |
In vitro | GPI-1046 is an analog of FK506, which is an immunophilin ligand that has been shown neuroprotective effects in neurodegenerative disease models [1]. GPI-1046 readily crosses the blood-brain barrier and promotes the regeneration of dopamine (DA) cells in the CNS in association with functional recovery in rodent models [2]. GPI-1046 improves the HIV-associated injury of peripheral nerves [3]. |
In vivo | Significant dose-dependent effects in the reduction of ethanol intake starting 48 h after the first treatment with GPI-1046 throughout treatment and post-treatment periods.?There were also dose-dependent increases in water intake.?However, GPI-1046 treatment did not affect the body weight of all animals nor sucrose intake.?Importantly, GPI-1046 (20mg/kg) increased GLT1 level compared to all groups in nucleus accumbens core (NAc-core).?Alternatively, GPI-1046 (10mg/kg) upregulated GLT1 level in NAc-core compared to vehicle (ethanol na?ve) group.?Moreover, both doses of GPI-1046 increased significantly GLT1 level in the prefrontal cortex (PFC) compared to ethanol na?ve vehicle group.?GPI-1046 (20mg/kg) increased GLT1 level in PFC compared to na?ve control group that was exposed to water and food only.?These findings demonstrated that neuroimmunophilin GPI-1046 attenuates ethanol intake in part through the upregulation of GLT1 in PFC and NAc-core[1]. |
Molecular Weight | 360.45 |
Formula | C20H28N2O4 |
Cas No. | 186452-09-5 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (277.43 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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