| Name | GPI-1046 |
| 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]. |
| Storage | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (9.16 mM), Sonication is recommended.
DMSO : 100 mg/mL (277.43 mM), Sonication is recommended.
|
| Keywords | Inhibitor | inhibit | Human immunodeficiency virus | HIVProtease | HIV Protease | HIV | GPI-1046 | GPI1046 | GPI 1046 | GLT1 | FKBP | FK506-binding protein |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Emtricitabine | Dolutegravir intermediate-1 | Dimethyl fumarate | Lamivudine | Valproic Acid | (-)-Epigallocatechin Gallate | Decanedioic acid | Dextran sulfate sodium salt (MW 5000) | Allyl Methyl Sulfide | Tenofovir |
| Related Compound Libraries | Bioactive Compound Library | ReFRAME Related Library | Antibiotics Library | Multi-Target Compound Library | Anti-Viral Compound Library | Neuroprotective Compound Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Anti-Infection Compound Library |
United States
