2. GPCR/G Protein Apoptosis
  3. Mas-related G-protein-coupled Receptor (MRGPR) TNF Receptor
  4. Z-3578

Z-3578 is an orally active small-molecule antagonist of MrgX2 with potent antipseudoallergic activity, exhibiting a KD value of 729 nM. Z-3578 effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, suppresses the release of β-hexosaminidase, significantly reduces the release of histamine and TNF-α, and decreases intracellular calcium flux. In a mouse pseudoallergy model, Z-3578 significantly alleviates paw swelling and dye extravasation, and reduces serum histamine levels. Z-3578 can be used for the study of pseudoallergic reactions.

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

Z-3578

Z-3578 Chemical Structure

CAS No. : 473687-20-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 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

Z-3578 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Z-3578

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Z-3578 is an orally active small-molecule antagonist of MrgX2 with potent antipseudoallergic activity, exhibiting a KD value of 729 nM. Z-3578 effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, suppresses the release of β-hexosaminidase, significantly reduces the release of histamine and TNF-α, and decreases intracellular calcium flux. In a mouse pseudoallergy model, Z-3578 significantly alleviates paw swelling and dye extravasation, and reduces serum histamine levels. Z-3578 can be used for the study of pseudoallergic reactions[1].

In Vitro

Z-3578 potently inhibits β-hexosaminidase release from human mast cell line LAD2 induced by SP (HY-P0201) and C48/80 (HY-130592), with IC50 values of 4.90 μM and 6.18 μM[1].
Z-3578 (1-10 μM) concentration-dependently inhibits SP-induced histamine release from LAD2 human mast cells[1].
Z-3578 (1-10 μM; 6 h) concentration-dependently inhibits SP-induced TNF-α release from human mast cell line LAD2[1].
Z-3578 (10 μM; 30 min) inhibits intracellular calcium mobilization in MrgX2-His-tag-HEK293 cells and blocks MrgX2-mediated signaling pathways[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Z-3578 Related Antibodies

ELISA Assay[1]

Cell Line: LAD2 human mast cell
Concentration: 1, 5 and 10 μM
Incubation Time: 6 h
Result: Reduced SP-induced TNF-α release in a concentration-dependent manner.
Showed significant inhibition at all tested concentrations.
In Vivo

Z-3578 (0.1-1 mg/mL, 1-10 mg/kg; i.g.; single dose) dose-dependently inhibits C48/80-induced pseudoallergic reactions in male C57BL/6 mice, with significant reductions in paw thickness, Evans blue extravasation, serum histamine release, and mast cell degranulation observed at doses of 0.5 mg/mL, 1 mg/mL, 5 mg/kg, and 10 mg/kg[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male, 6-8 weeks old)[1]
Dosage: 0.1 mg/mL; 0.5 mg/mL; 1 mg/mL; 1 mg/kg; 5 mg/kg; 10 mg/kg
Administration: i.g.; single dose
Result: Significantly reduced paw edema induced by C48/80 in mice at concentrations of 0.5 and 1.0 mg/mL.
Significantly decreased Evans blue extravasation at a concentration of 1.0 mg/mL.
Markedly lowered serum histamine release induced by C48/80.
Attenuated mast cell degranulation in the mouse paw skin induced by C48/80.
Molecular Weight

467.37

Formula

C23H16Cl2N4OS
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(CSC1=NC(C2=CC=CC=C2)=C(N=N1)C3=CC=CC=C3)NC4=C(C=C(C=C4)Cl)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (53.49 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 2.1396 mL 10.6982 mL 21.3963 mL
5 mM 0.4279 mL 2.1396 mL 4.2793 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 (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.

  • 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 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.
Calculation results:
Working solution concentration: mg/mL
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 (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
DMSO 1 mM 2.1396 mL 10.6982 mL 21.3963 mL 53.4908 mL
5 mM 0.4279 mL 2.1396 mL 4.2793 mL 10.6982 mL
10 mM 0.2140 mL 1.0698 mL 2.1396 mL 5.3491 mL
15 mM 0.1426 mL 0.7132 mL 1.4264 mL 3.5661 mL
20 mM 0.1070 mL 0.5349 mL 1.0698 mL 2.6745 mL
25 mM 0.0856 mL 0.4279 mL 0.8559 mL 2.1396 mL
30 mM 0.0713 mL 0.3566 mL 0.7132 mL 1.7830 mL
40 mM 0.0535 mL 0.2675 mL 0.5349 mL 1.3373 mL
50 mM 0.0428 mL 0.2140 mL 0.4279 mL 1.0698 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.

Z-3578 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:

Z-3578473687-20-6Z3578Z 3578Mas-related G-protein-coupled Receptor (MRGPR)TNF ReceptorTumor Necrosis Factor ReceptorTNFRmast cell degranulationinflammatory mediator releasepseudoallergymale C57BL/6 miceMrgX2-His-tag-HEK293 cellsLAD2 human mast cellsMrgX2Evans blue extravasationpaw swellingcalcium mobilizationInhibitorinhibitorinhibit

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:
Z-3578
Cat. No.:
HY-172458
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 (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB) Italian - IT (252 KB) Korean - KR (252 KB) Portuguese - PT (252 KB)

Request for HNMR Report

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