γ-Glu-Tyr
Based on 1 publication(s) in Google Scholar
γ-Glu-Tyr is an orally active gut microbiota-derived metabolite and a competitive DPP-IV inhibitor with an IC50 of 6.77 mM against hDPP-IV. γ-Glu-Tyr weakly activates hCaSR. γ-Glu-Tyr decreases colonic pro-inflammatory cytokine (IL-6, IL-1β, TNF-α) levels. γ-Glu-Tyr activates the cAMP/PKA signaling pathway and inhibits NF-κB phosphorylation, thereby reducing inflammatory responses. γ-Glu-Tyr can be used for research on type 2 diabetes and ulcerative colitis.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.37%
- CAS. Nr.: 7432-23-7
- Formel: C14H18N2O6
- Molecular Weight:310.30
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Speicherung:
Sealed storage, away from moisture and light.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) γ-Glu-Tyr
MoreAlle Endogenous Metabolite Isoform-spezifische Produkte anzeigen
MoreAlle TNF Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
Beschreibung
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DPP-4 6.774 mM (IC50) |
Microbial Metabolite |
IL-6 |
IL-1β |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | EC50 |
508 μM
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Activation of hCaSR in HEK293T cells cotransfected with hCaSR and hGα15 assessed as increase in intracellular Ca2+ levels measured by Fluo-8 AM fluorescence.
Activation of hCaSR in HEK293T cells cotransfected with hCaSR and hGα15 assessed as increase in intracellular Ca2+ levels measured by Fluo-8 AM fluorescence.
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32202205 |
In Vitro
γ-Glu-Tyr (0.0125-2.5 mg/mL; 30 min) acts as a competitive inhibitor of human DPP-IV with an IC50 of 6.774 mM[1].
γ-Glu-Tyr weakly activates hCaSR in HEK293T cells with an EC50 of 508 μM, confirming that the γ-glutamyl moiety in the N-terminus and Tyr residue in the C-terminus contribute to its potency[2].
γ-Glu-Tyr (0-75 μM; 24 h) is non-cytotoxic up to 75 μM and optimally reduces IL-1β release at 50 μM in LPS-stimulated RAW264.7 cells[3].
γ-Glu-Tyr (50 μM; 24 h) inhibits IL-1β release in LPS-stimulated RAW264.7 cells by activating the cAMP/PKA/NF-κB pathway[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7
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Concentration:0-75 μM
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Incubation Time:24 h
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Result:Demonstrated non-cytotoxicity up to 75 μM.
Showed optimal reduction of IL-1β levels at 50 μM compared with the 0 μM control.
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Cell Line:RAW264.7
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Concentration:50 μM
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Incubation Time:24 h
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Result:Increased p-PKA expression (0.72 vs.
LPS: 0.16).
Decreased p-NF-κB expression (0.21 vs.
LPS: 0.95).
In Vivo
γ-Glu-Tyr (50 mg/kg; i.g.; daily; 10 days) protects mice against DSS-induced ulcerative colitis by activating the cAMP/PKA/NF-κB pathway[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 6 weeks old, 20-24 g, DSS-induced)[3]
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Dosage:50 mg/kg
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Administration:i.g.; daily; 10 days
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Result:Significantly improved body weight.
Decreased DAI scores.
Increased colon length.
Mitigated colonic histopathological damage and inflammation.
Decreased colonic levels of IL-6, IL-1β, and TNF-α.
Decreased levels of γ-linolenic acid.
Increased cAMP levels and p-PKA expression (0.81 vs.
DSS: 0.15).
Decreased p-NF-κB levels (0.19 vs.
DSS: 0.76).
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Animal Model:C57BL/6 (male, 6 weeks old, 20-24 g, antibiotic cocktail pretreatment followed by DSS-induced)[3]
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Dosage:50 mg/kg (combined with 80 mg/kg AA)
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Administration:i.g.; daily; 10 days
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Result:Significantly enhanced the beneficial effects of AA on DSS-induced body weight loss, colon length shortening, and colonic pathological changes and inflammation.
Decreased levels of γ-linolenic acid in the colon.
Reversed the negative regulatory effects of DSS on the cAMP/PKA/NF-κB pathway by increasing cAMP and p-PKA levels and decreasing p-NF-κB levels.
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Animal Model:C57BL/6 (male, 6 weeks old, 20-24 g, DSS-induced)[3]
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Dosage:50 mg/kg (γ-Glu-Tyr); 10 mg/kg (H-89); 1 mg/kg (NF-κB activator 2)
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Administration:i.g. (daily, 10 days); s.c. (daily, 10 days); i.p. (daily, 10 days)
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Result:Increased cAMP levels and p-PKA expression.
Decreased p-NF-κB expression.
Co-treatment with H-89 reversed the γ-Glu-Tyr-induced increase in p-PKA (0.24 vs. γ-Glu-Tyr: 0.85) and p-NF-κB (0.66 vs. γ-Glu-Tyr: 0.12).
NF-κB activator 2 reversed the suppression of p-NF-κB expression (0.81 vs. γ-Glu-Tyr: 0.12).
Attenuated protective effects against DSS-induced reductions in body weight, increases in DAI scores, decreases in colon length, and improvements in colonic pathological damage and inflammation following co-treatment with either H-89 or NF-κB activator 2.
Chemical Information
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CAS. Nr. 7432-23-7
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Appearance Solid
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Molecular Weight 310.30
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Formel C14H18N2O6
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Color White to off-white
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Sequence
{γ-Glu}-Tyr
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Sequence Shortening
{γ-Glu}-Y
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Sealed storage, away from moisture and light
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (322.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 12.5 mg/mL (40.28 mM; Need ultrasonic)
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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
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: ≥ 2.5 mg/mL (8.06 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (8.06 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
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 (sealed storage, away from moisture and 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.
Reinheit & Dokumentation
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Data Sheet (292 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
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 (sealed storage, away from moisture and 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.2227 mL | 16.1134 mL | 32.2269 mL | 80.5672 mL |
| 5 mM | 0.6445 mL | 3.2227 mL | 6.4454 mL | 16.1134 mL | |
| 10 mM | 0.3223 mL | 1.6113 mL | 3.2227 mL | 8.0567 mL | |
| 15 mM | 0.2148 mL | 1.0742 mL | 2.1485 mL | 5.3711 mL | |
| 20 mM | 0.1611 mL | 0.8057 mL | 1.6113 mL | 4.0284 mL | |
| 25 mM | 0.1289 mL | 0.6445 mL | 1.2891 mL | 3.2227 mL | |
| 30 mM | 0.1074 mL | 0.5371 mL | 1.0742 mL | 2.6856 mL | |
| 40 mM | 0.0806 mL | 0.4028 mL | 0.8057 mL | 2.0142 mL | |
| DMSO | 50 mM | 0.0645 mL | 0.3223 mL | 0.6445 mL | 1.6113 mL |
| 60 mM | 0.0537 mL | 0.2686 mL | 0.5371 mL | 1.3428 mL | |
| 80 mM | 0.0403 mL | 0.2014 mL | 0.4028 mL | 1.0071 mL | |
| 100 mM | 0.0322 mL | 0.1611 mL | 0.3223 mL | 0.8057 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
γ-Glu-Tyr Related Classifications
HY-P4633 Related Classifications
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Keywords
- γ-Glu-Tyr
- 7432-23-7
- Dipeptidyl Peptidase
- Endogenous Metabolite
- CaSR
- Interleukin Related
- TNF Receptor
- PKA
- NF-κB
- competitive inhibitor
- human calcium-sensing receptor
- kokumi
- cAMP/PKA signaling pathway
- ulcerative colitis
- gut microbiota-derived metabolite
- dipeptidyl peptidase-IV
- orthosteric agonist
- positive allosteric modulator
- Inhibitor
- inhibitor
- inhibit