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GPI-1046
Catalog No. T11451Cas No. 186452-09-5
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.
GPI-1046
Catalog No. T11451Cas No. 186452-09-5
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.
| 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 |
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Purity:99.91%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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 & Solubility Information
| 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 | ||||||||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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