1. Apoptosis
    Immunology/Inflammation
    Autophagy
    Anti-infection
  2. FKBP
    HIV
  3. GPI-1046

GPI-1046 

Cat. No.: HY-124619 Purity: 99.43%
Handling Instructions

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.

For research use only. We do not sell to patients.

GPI-1046 Chemical Structure

GPI-1046 Chemical Structure

CAS No. : 186452-09-5

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 143 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 300 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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[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[1]

GLT1

 

Molecular Weight

360.45

Formula

C₂₀H₂₈N₂O₄

CAS No.

186452-09-5

SMILES

O=C(OCCCC1=CC=CN=C1)[[email protected]]2N(C(C(C(C)(C)CC)=O)=O)CCC2

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
In Vitro: 

DMSO : ≥ 100 mg/mL (277.43 mM)

*"≥" means soluble, but saturation unknown.

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (2.77 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1 mg/mL (2.77 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (2.77 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

GPI-1046GPI1046GPI 1046FKBPHIVFK506-binding proteinHuman immunodeficiency virusInhibitorinhibitorinhibit

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GPI-1046
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