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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

GPI-1046

Purity: 99.91%
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 SizePriceAvailabilityQuantity
1 mg$41In Stock
5 mg$88In Stock
10 mg$148In Stock
25 mg$251In Stock
50 mg$358In Stock
100 mg$518In Stock
200 mg$715In Stock
1 mL x 10 mM (in DMSO)$80In Stock
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Purity:99.91%
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight360.45
FormulaC20H28N2O4
Cas No.186452-09-5
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.7743 mL13.8715 mL27.7431 mL138.7155 mL
5 mM0.5549 mL2.7743 mL5.5486 mL27.7431 mL
10 mM0.2774 mL1.3872 mL2.7743 mL13.8715 mL
20 mM0.1387 mL0.6936 mL1.3872 mL6.9358 mL
50 mM0.0555 mL0.2774 mL0.5549 mL2.7743 mL
100 mM0.0277 mL0.1387 mL0.2774 mL1.3872 mL

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