2. GPCR/G Protein Immunology/Inflammation Apoptosis PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway
  3. Mas-related G-protein-coupled Receptor (MRGPR) Interleukin Related TNF Receptor Akt ERK
  4. GE1111

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.

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

GE1111

GE1111 Chemical Structure

CAS No. : 2883669-12-1

Size Price Stock Quantity
1 mg In-stock
5 mg In-stock
10 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

GE1111 Related Antibodies

Top Publications Citing Use of Products

View All Interleukin Related Isoform Specific Products:

View All Isoforms
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

View All TNF Receptor Isoform Specific Products:

View All Isoforms
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3].

IC50 & Target

IC50: 9.42 μM (MRGPRX2)
In Vitro

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.

GE1111 Related Antibodies

Western Blot Analysis[1]

Cell Line: LAD2 cells
Concentration: 50 μM
Incubation Time: 30 min
Result: Reduced pERK1/2 levels compared to control when treated alone.
Significantly inhibited agonist-induced increases in pERK1/2 phosphorylation and STIM1 expression.

Immunofluorescence[1]

Cell Line: LAD-2 MCs and
HaCaT keratinocytes
Concentration: 50 μM
Incubation Time: 2 h
Result: Increased claudin 1 expression and Reduced TSLP expression.

Western Blot Analysis[1]

Cell Line: LAD-2 MCs and HaCaT keratinocytes
Concentration: 50 μM
Incubation Time: 2 h
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.

Immunofluorescence[1]

Cell Line: LAD-2 MCs and RAW 264.7 cells
Concentration: 50 μM
Incubation Time: 2 h
Result: Mitigated the
negative effects of LL-37 on macrophage function.
In Vivo

GE1111 (10-20 mg/kg; i.p.; daily; 6 days) alleviates LL-37-induced rosacea-like inflammation in mice by inhibiting mast cell degranulation, restoring skin barrier function, and reducing systemic and local inflammatory mediators[1].
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.

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]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.p.; daily; 6 days
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.
Animal Model: C57BL/6N wild-type adult male; MRGPRB2 knock-out adult male (compound 48/80-induced itch model)[1]
Dosage: 20 mg/kg
Administration: i.p.; single dose 30 minutes prior to compound 48/80 injection
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.
Animal Model: BALB/c (male, 6 to 8 weeks old, DNFB-induced atopic dermatitis)[2]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.p.; once weekly; 4 weeks
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.
Animal Model: C57BL/6N (adult male, 6-8 weeks old, 2.5-4% dextran sulfate sodium-induced colitis)[3]
Dosage: 300 µg/kg
Administration: i.p.; every alternative day; Day 0 to Day 12
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.
Molecular Weight

466.48

Formula

C28H22N2O5
CAS No.
Appearance

Solid

Color

Yellow to orange

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1437 mL 10.7186 mL 21.4371 mL
5 mM 0.4287 mL 2.1437 mL 4.2874 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

GE1111 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GE11112883669-12-1GE 1111GE-1111Mas-related G-protein-coupled Receptor (MRGPR)Interleukin RelatedTNF ReceptorAktERKILTumor Necrosis Factor ReceptorTNFRPKBProtein kinase BExtracellular signal regulated kinasesMRGPRX2 antagonistLAD2 cellsHaCaT cellsRAW 264.7 cellsC57BL/6N miceBALB/c micerosaceaatopic dermatitisulcerative colitis
Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GE1111
Cat. No.:
HY-158990
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

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)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.