GE1111
Based on 1 Customer Validation
GE1111 is a MRGPRX2 antagonist (IC50 = 9.4 μM). GE1111 inhibits MRGPRX2/MRGPRB2-mediated mast cell activation. GE1111 reduces the expressions of TSLP, IL-13, MCP-1, TNF-α, IL-1β and periostin, maintains the expression levels of claudin 1 and involucrin, restores the phagocytic activity of macrophages, and attenuates the activation of STIM1 and phosphorylated AKT. GE1111 exerts anti-inflammatory and anti-allergic effects in multiple animal models. GE1111 is applicable to the research related to rosacea, atopic dermatitis and ulcerative colitis.
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- Pureza: 95.73%
- No. CAS: 2883669-12-1
- Fòrmula: C28H22N2O5
- Peso molecular:466.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
IC50: 9.42 μM (MRGPRX2)
GE1111 potently inhibits LL-37-induced degranulation of LAD-2 human mast cells, with an IC50 value of 6.271 μM[1].
GE1111 (30 min) inhibits LL-37-induced MRGPRX2-mediated calcium influx in MRGPRX2-transfected HEK-293 cells, with an IC50 of 12.31 μM[1].
GE1111 (50 μM; 30 min) inhibits the activation of LL-37-induced MRGPRX2 downstream signaling pathways (STIM1, ERK 1/2) and reduces the expression of pro-inflammatory cytokine genes (IL-31, MCP-1, TNF-α) in human mast cell line LAD-2[1].
GE1111 (50 μM; 2 h) restores claudin-1 expression, reduces the expression of pro-inflammatory TSLP, and downregulates the expression of pro-inflammatory cytokine genes (IL-8, IL-13, IL-17) in human keratinocyte HaCaT cells exposed to mast cell-conditioned medium[1].
GE1111 (50 μM; 2 h) restores the phagocytic function of RAW 264.7 mouse macrophages impaired by mast cell conditioned medium stimulated with LL-37[1].
GE1111 (0.01 nM-100 μM; 1 h) acts as an inverse agonist and antagonist of MRGPRX2 in Mrgprx2-transfected HTLA cells, reducing both basal β-arrestin recruitment levels and agonist-induced β-arrestin recruitment levels[3].
GE1111 (100 μM; 1 h) induces internalization of MRGPRX2 in LAD2 mast cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LAD2 cells
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Concentration:50 μM
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Incubation Time:30 min
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Result:Reduced pERK1/2 levels compared to control when treated alone.
Significantly inhibited agonist-induced increases in pERK1/2 phosphorylation and STIM1 expression.
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Cell Line:LAD-2 MCs and
HaCaT keratinocytes -
Concentration:50 μM
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Incubation Time:2 h
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Result:Increased claudin 1 expression and Reduced TSLP expression.
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Cell Line:LAD-2 MCs and HaCaT keratinocytes
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Concentration:50 μM
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Incubation Time:2 h
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Result:Exhibited a significant reduction
in the gene expression of inflammatory cytokines induced
by LL-37, compared to the group treated only with LL-37
MCs supernatant IL-8, IL-13 and IL-17.
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Cell Line:LAD-2 MCs and RAW 264.7 cells
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Concentration:50 μM
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Incubation Time:2 h
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Result:Mitigated the
negative effects of LL-37 on macrophage function.
GE1111 (20 mg/kg; i.p.; single pre-treatment) alleviates compound 48/80 (HY-115768)-induced pruritus in mice by inhibiting mast cell degranulation[1].
GE1111 (10-20 mg/kg; i.p.; weekly; for 4 consecutive weeks) significantly alleviates DNFB-induced atopic dermatitis in mice by reducing skin inflammation, inhibiting mast cell degranulation, downregulating the expression of inflammatory mediators, and restoring the expression of epidermal barrier proteins[2].
GE1111 (300 µg/kg; i.p.; once every other day for 12 days) improves the survival rate of C57BL/6N mice with ulcerative colitis induced by 4% DSS (HY-116282C). It alleviates the disease severity of C57BL/6N mice with ulcerative colitis induced by 2.5% DSS by restoring colonic integrity, normalizing cytokine levels, reducing immune cell infiltration, and decreasing the colonic expression of Mrgprb2/Mrgpra1[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6N wild-type adult male (6 to 8 weeks old, LL-37-induced rosacea model); MRGPRB2 knock-out adult male (6 to 8 weeks old, LL-37-induced rosacea model)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; daily; 6 days
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Result:Reduced skin redness/damage severity scores.
Reduced serum MCP-1 levels, epidermal thickness, and the percentage of degranulated mast cells in skin tissue.
Restored the expression of epidermal barrier proteins involucrin and claudin-1, and reduces the expression of STIM1 and TSLP proteins.
Reduced gene expression of inflammatory cytokines IL-13, IL-33, MCP-1, IL-1β, and TNF-α in skin tissue.
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Animal Model:C57BL/6N wild-type adult male; MRGPRB2 knock-out adult male (compound 48/80-induced itch model)[1]
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Dosage:20 mg/kg
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Administration:i.p.; single dose 30 minutes prior to compound 48/80 injection
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Result:Reduced the number and total duration of scratching episodes compared to compound 48/80-treated control mice, without affecting the average length of individual scratches.
Reduced the percentage of degranulated mast cells in skin tissue relative to compound 48/80-treated controls.
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Animal Model:BALB/c (male, 6 to 8 weeks old, DNFB-induced atopic dermatitis)[2]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; once weekly; 4 weeks
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Result:Reduced skin thickening scores, erythema scores, and epidermal thickness in the skin and ear.
Significantly reduced skin scaling scores in the 10 mg/kg dose group.
Reduced serum MCP-1 levels and skin TSLP protein expression in the 20 mg/kg dose group.
Reduced the percentage of degranulated mast cells in ear tissue, maintained skin capsule protein expression, and reduced skin periosteal protein expression.
Reduced gene expression of TSLP, IL-13, and IL-1β in the skin, and reduced protein expression of STIM1 and p-AKT in the skin.
Significantly increased claudin 1 protein expression in the skin.
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Animal Model:C57BL/6N (adult male, 6-8 weeks old, 2.5-4% dextran sulfate sodium-induced colitis)[3]
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Dosage:300 µg/kg
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Administration:i.p.; every alternative day; Day 0 to Day 12
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Result:Increased the survival rate of mice subjected to 4% DSS-induced colitis.
Reduced body weight and Disease Activity Index (DAI) score.
Restored colon length, reduced colon weight/length ratio, and decreased intestinal permeability (reduced FITC-glucan fluorescence intensity in plasma).
Reduced colonic erosion and histological damage, restored colonic integrity genes claudin 1, occludin, and E-cadherin mRNA expression, and reduced VEGF mRNA expression.
Restored claudin 1 protein expression in colonic tissue, reduced plasma M-CSF, G-CSF, and BLC concentrations, and partially restored plasma sTNF RI concentration.
Reduced CD68+ and F4/80+ immune cell infiltration in the colon and reduced colonic COX-2 expression.
Reduced Mrgpra1 and Mrgprb2 mRNA expression in colonic tissue.
Chemical Information
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No. CAS 2883669-12-1
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Appearance Solid
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Peso molecular 466.48
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Fòrmula C28H22N2O5
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Color Yellow to orange
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SMILES
O=CC1=CC2=C3C(C1C)=C(O)C=CC3=CC(C4=CC5=C(C=C4C(OC)=O)C=C(NC(N)=O)C=C5)=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (214.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. 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. 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: ≥ 5 mg/mL (10.72 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (10.72 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Pureza y Documentación
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Ficha de datos (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Chow BKC, et al. Therapeutic effect of an MRGPRX2/MRGPRB2 antagonist on LL-37-induced rosacea-like inflammation in mice. Inflamm Res. 2025;74(1):174. Published 2025 Nov 26. [Content Brief]
[2]. Wong TK, et al. MRGPRX2 antagonist GE1111 attenuated DNFB-induced atopic dermatitis in mice by reducing inflammatory cytokines and restoring skin integrity. Front Immunol. 2024;15:1406438. Published 2024 May 16. [Content Brief]
[3]. Duraisamy K, et al. MRGPRB2/X2 and the analogous effects of its agonist and antagonist in DSS-induced colitis in mice. Biomed Pharmacother. 2024;174:116471. [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. 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 | 2.1437 mL | 10.7186 mL | 21.4371 mL | 53.5929 mL |
| 5 mM | 0.4287 mL | 2.1437 mL | 4.2874 mL | 10.7186 mL | |
| 10 mM | 0.2144 mL | 1.0719 mL | 2.1437 mL | 5.3593 mL | |
| 15 mM | 0.1429 mL | 0.7146 mL | 1.4291 mL | 3.5729 mL | |
| 20 mM | 0.1072 mL | 0.5359 mL | 1.0719 mL | 2.6796 mL | |
| 25 mM | 0.0857 mL | 0.4287 mL | 0.8575 mL | 2.1437 mL | |
| 30 mM | 0.0715 mL | 0.3573 mL | 0.7146 mL | 1.7864 mL | |
| 40 mM | 0.0536 mL | 0.2680 mL | 0.5359 mL | 1.3398 mL | |
| 50 mM | 0.0429 mL | 0.2144 mL | 0.4287 mL | 1.0719 mL | |
| 60 mM | 0.0357 mL | 0.1786 mL | 0.3573 mL | 0.8932 mL | |
| 80 mM | 0.0268 mL | 0.1340 mL | 0.2680 mL | 0.6699 mL | |
| 100 mM | 0.0214 mL | 0.1072 mL | 0.2144 mL | 0.5359 mL |
GE1111 Related Classifications
HY-158990 Related Classifications
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