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GPI-1046

Catalog No. T11451 CAS 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.

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GPI-1046, CAS 186452-09-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 68.00
2 mg	In stock	$ 95.00
5 mg	In stock	$ 147.00
10 mg	In stock	$ 247.00
25 mg	In stock	$ 418.00
50 mg	In stock	$ 596.00
100 mg	In stock	$ 863.00
1 mL * 10 mM (in DMSO)	In stock	$ 133.00

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Purity: 99.91%

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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

Solubility Information

DMSO: 100 mg/mL (277.43 mM)

References and Literature

1. Sari Y, et al. Neuroimmunophilin GPI-1046 reduces ethanol consumption in part through activation of GLT1 in alcohol-preferring rats. Neuroscience. 2012 Dec 27;227:327-35. 2. Eberling JL, et al. The immunophilin ligand GPI-1046 does not have neuroregenerative effects in MPTP-treated monkeys. Exp Neurol. 2002 Dec;178(2):236-42.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Infection Compound Library Immunology/Inflammation Compound Library Apoptosis Compound Library Covalent Inhibitor Library Bioactive Compounds Library Max ReFRAME Related Library Antibiotics Library Bioactive Compound Library Anti-Viral Compound Library NO PAINS Compound Library

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Keywords

GPI-1046 186452-09-5 Microbiology/Virology Others Proteases/Proteasome HIV Protease GPI1046 Human immunodeficiency virus FKBP GPI 1046 FK506-binding protein inhibit HIV Inhibitor inhibitor

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