2. GPCR/G Protein
  3. Mas-related G-protein-coupled Receptor (MRGPR)
  4. HEP-50768

HEP-50768 is an orally active and selective MRGPRX4 (hX4) antagonist. HEP-50768 suppresses basal and bile-acid-stimulated hX4 activity. HEP-50768 binds the receptor’s transmembrane pocket and induces extracellular loop rearrangements. HEP-50768 modulates GPCR microswitch motifs and reduces bile-acid-induced pruritic scratching behaviors. HEP-50768 can be used for the research of cholestatic pruritus.

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

HEP-50768

HEP-50768 Chemical Structure

CAS No. : 3036387-75-1

Size Stock
1 mg Check price and availability
5 mg Check price and availability
10 mg Check price and availability

* Please select Quantity before adding items.

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

HEP-50768 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

HEP-50768 is an orally active and selective MRGPRX4 (hX4) antagonist. HEP-50768 suppresses basal and bile-acid-stimulated hX4 activity. HEP-50768 binds the receptor’s transmembrane pocket and induces extracellular loop rearrangements. HEP-50768 modulates GPCR microswitch motifs and reduces bile-acid-induced pruritic scratching behaviors. HEP-50768 can be used for the research of cholestatic pruritus[1].

In Vitro

HEP-50768 (1 nM-1 μM; 30 min) potently inhibits DCA-induced calcium mobilization in HEK293T cells stably expressing hX4 with an IC50 of 14 nM and achieves 100% inhibition at 2 μM[1].
HEP-50768 (0.1 μM) acts as an inverse agonist, significantly reducing basal inositol monophosphate levels in HEK293T cells expressing hX4[1].
HEP-50768 (2 μM; 1.5 h) modestly reduces GTPase activity of the purified hX4-Gq complex, consistent with its inverse agonist activity[1].
HEP-50768 (0.02-50 nM) binds purified apo hX4 and hX4-miniGαq complex with high, comparable affinity, exhibiting K0 values of 0.6 nM and 0.7 nM, respectively[1].
HEP-50768 (0.1 nM-10 mM; 30 min) is highly selective for hX4, showing weak inhibition of hX1 (IC50 = 16 μM) and hX2 (IC50 = 1.5 μM) with no agonist activity against either receptor[1].
HEP-50768 (~5 min) shows minimal hERG channel inhibition in HEK293 cells stably expressing hERG, with an IC50 exceeding 30 μM[1].

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

HEP-50768 Related Antibodies
In Vivo

HEP-50768 (5-10 mg/kg; p.o.; single dose; 2.5 hours before pruritus induction) significantly reduces DCA-3S-induced scratching behavior in hX4-humanized rats, demonstrating potent antipruritic efficacy[1].

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

Animal Model: hX4-humanized rats (generated by crossing MRGA::hX4-Cre rats with Rosa26::lsl-hX4 rats)[1]
Dosage: 5 mg/kg; 10 mg/kg
Administration: p.o.; single dose; 2.5 hours before pruritus induction
Result: Significantly reduced DCA-3S-induced scratching bouts compared to PBS vehicle control with a P-value of 0.0059 (5 mg/kg dose).
Significantly reduced DCA-3S-induced scratching bouts compared to PBS vehicle control with a P-value of 0.0049 (10 mg/kg dose).
Molecular Weight

350.27

Formula

C16H10F4N4O
CAS No.
SMILES

FC1=C(C2=NN=NN2)C=CC=C1[C@@H]3CC4=CC(C(F)(F)F)=CC=C4O3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • 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.

HEP-50768 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

HEP-507683036387-75-1HEP50768HEP 50768Mas-related G-protein-coupled Receptor (MRGPR)HEK293 cellshERG channelcholestatic pruritushX2hX4GTPaseinositol monophosphateHEK293T cellsMRGPRX4hX1Inhibitorinhibitorinhibit

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:
HEP-50768
Cat. No.:
HY-183050
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)

Request for HNMR Report

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