MedChemExpress - Model GPI-1046 - 186452-09-5
GPI-1046 is a 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 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 HIV-associated injury of peripheral nerves[3].MCE products for research use only. We do not sell to patients.
GPI-1046
MCE China：GPI-1046
Brand：MedChemExpress (MCE)
Cat. No.HY-124619
CAS：186452-09-5
Purity：99.74%
Storage：4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Shipping：Room temperature in continental US; may vary elsewhere.
Description：GPI-1046 is a 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 is an analog of FK506, which is an immunophilin ligand that has been shown neuroprotective effects in neurodegenerative disease models. 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. GPI-1046 improves HIV-associated injury of peripheral nerves.
IC50 & Target：GLT1
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References：
[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. [Content Brief]
[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. [Content Brief]
[3]. Scott Letendre, et al. Neurologic Complications of HIV Disease and Their Treatment. Top HIV Med. Apr-May 2007;15(2):32-9. [Content Brief]
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