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[CAS NO. 186452-09-5] GPI-1046
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-124619 |
| Brand: | MCE |
| CAS: | 186452-09-5 |
Overview
| MDL | MFCD00953146 |
|---|---|
| Molecular Weight | 360.45 |
| Molecular Formula | C20H28N2O4 |
| SMILES | O=C(OCCCC1=CC=CN=C1)[C@H]2N(C(C(C(C)(C)CC)=O)=O)CCC2 |
Summary
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] .
IC50 & Target
|
GLT1
|
Appearance
Liquid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 277.43 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7743 mL | 13.8715 mL | 27.7431 mL |
| 5 mM | 0.5549 mL | 2.7743 mL | 5.5486 mL |
| 10 mM | 0.2774 mL | 1.3872 mL | 2.7743 mL |
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.
- [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.
- [3] Scott Letendre, et al. Neurologic Complications of HIV Disease and Their Treatment. Top HIV Med. Apr-May 2007;15(2):32-9.
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