GPI-1046
Based on 1 Customer Validation
GPI-1046 is an orally active, antibiotic-free immunophilin ligand that reduces ethanol intake by upregulating glutamate transporter 1 (GLT1) in the prefrontal cortex (PFC) and nucleus accumbens core (NAc-core). GPI-1046 improves human immunodeficiency virus (HIV)-associated sensory neuropathy (HIV-SN) by attenuating store-operated calcium (SOC) entry. GPI-1046 has neuroprotective activity.
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- Pureté: 99.79%
- CAS No.: 186452-09-5
- Formule: C20H28N2O4
- Masse moléculaire:360.45
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Activité biologique
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GLT1 |
GPI-1046 (1-1000 nM, 15 hours) protects neurites from damage in a dose-dependent manner in gp120-induced dorsal root ganglion (DRG) neurons[2].
GPI-1046 (100 nM) protects gp120-induced DRG neurons from neurite damage by reducing IP3 receptor-mediated calcium release through lowering endoplasmic reticulum calcium and reducing calcium ion entry into cells by SOC[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GPI-1046 (50 mg/kg, p.o., once a day, for 1-4 weeks) significantly raises the expression and function of GLT1 and has a neuroprotective effect[3].
GPI-1046 (50 mg/kg, p.o., twice a day, until death) effectively prolongs the survival of mice with amyotrophic lateral sclerosis (ALS) and significantly increases the level of GLT1 protein[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Alcohol-preferring rats (male aged 3 weeks) [1]
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Dosage:10, 20 mg/kg
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Administration:i.p., once a day, 8 days
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Result:Reduced ethanol intake in a dose-dependent manner, the higher dose (20 mg/kg) significantly reduced ethanol intake (70% reduction).
Upregulated GLT1 levels in the NAc-core and significantly increased GLT1 levels in the prefrontal cortex (PFC).
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Animal Model:G93A transgenic SOD1 mice [3]
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Dosage:50 mg/kg
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Administration:p.o., twice a day, until death
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Result:Showed an average survival of 240.5 days, significantly longer than the control group (214.6 days), an increase of approximately 12% (26 days).
Did not significantly improve motor function decline, but prolonged survival indicated that it slowed disease progression.
Significantly increases GLT1 protein levels.
Chemical Information
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CAS No. 186452-09-5
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Appearance Liquid (Density: 1.143±0.06 g/cm3)
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Masse moléculaire 360.45
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Formule C20H28N2O4
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Color Colorless to light yellow
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SMILES
O=C(OCCCC1=CC=CN=C1)[C@H]2N(C(C(C(C)(C)CC)=O)=O)CCC2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
DMSO : ≥ 100 mg/mL (277.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.77 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.77 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[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]. Höke A, et al. GPI-1046 protects dorsal root ganglia from gp120-induced axonal injury by modulating store-operated calcium entry. J Peripher Nerv Syst. 2009 Mar;14(1):27-35. [Content Brief]
[3]. Ganel R, et al. Selective up-regulation of the glial Na+-dependent glutamate transporter GLT1 by a neuroimmunophilin ligand results in neuroprotection. Neurobiol Dis. 2006 Mar;21(3):556-67. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7743 mL | 13.8715 mL | 27.7431 mL | 69.3577 mL |
| 5 mM | 0.5549 mL | 2.7743 mL | 5.5486 mL | 13.8715 mL | |
| 10 mM | 0.2774 mL | 1.3872 mL | 2.7743 mL | 6.9358 mL | |
| 15 mM | 0.1850 mL | 0.9248 mL | 1.8495 mL | 4.6238 mL | |
| 20 mM | 0.1387 mL | 0.6936 mL | 1.3872 mL | 3.4679 mL | |
| 25 mM | 0.1110 mL | 0.5549 mL | 1.1097 mL | 2.7743 mL | |
| 30 mM | 0.0925 mL | 0.4624 mL | 0.9248 mL | 2.3119 mL | |
| 40 mM | 0.0694 mL | 0.3468 mL | 0.6936 mL | 1.7339 mL | |
| 50 mM | 0.0555 mL | 0.2774 mL | 0.5549 mL | 1.3872 mL | |
| 60 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1560 mL | |
| 80 mM | 0.0347 mL | 0.1734 mL | 0.3468 mL | 0.8670 mL | |
| 100 mM | 0.0277 mL | 0.1387 mL | 0.2774 mL | 0.6936 mL |
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