2. GPCR/G Protein Apoptosis Immunology/Inflammation
  3. GPR68 TNF Receptor Interleukin Related
  4. GPR68 antagonist 1

GPR68 antagonist 1 is a GPR68 antagonist with an IC50 of 81 nM. GPR68 antagonist 1 inhibits the mouse GPR68-mediated cAMP signaling pathway with an IC50 of 179 nM. GPR68 antagonist 1 alleviates disease symptoms in a dextran sulfate sodium (DSS) (HY-116282C)-induced mouse model of inflammatory bowel disease. GPR68 antagonist 1 is applicable to research related to inflammatory bowel disease.

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

GPR68 antagonist 1

GPR68 antagonist 1 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

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

GPR68 antagonist 1 Related Antibodies

Top Publications Citing Use of Products

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 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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GPR68 antagonist 1 is a GPR68 antagonist with an IC50 of 81 nM. GPR68 antagonist 1 inhibits the mouse GPR68-mediated cAMP signaling pathway with an IC50 of 179 nM. GPR68 antagonist 1 alleviates disease symptoms in a dextran sulfate sodium (DSS) (HY-116282C)-induced mouse model of inflammatory bowel disease. GPR68 antagonist 1 is applicable to research related to inflammatory bowel disease[1].

IC50 & Target[1]

IL-6

 

IL-1β

 

Parmacokinetics
Species Dose Route Cmax Tmax T1/2 CLz/F Vz/F AUC0-t Bioavailability
Mice[1] 30 mg/kg i.p. 1889.06 ng/mL 2.00 h 3.21 h 2.45 mL/min/kg 11.40 L/kg 12243.55 ng·h/mL /
Mice[1] 30 mg/kg p.o. 182.91 ng/mL 0.50 h 2.73 h 51.20 mL/min/kg 203.18 L/kg 552.49 ng·h/mL 2.36 %
Mice[1] 10 mg/kg i.v. 1774.50 ng/mL 0.08 h 2.51 h 1.28 mL/min/kg 4.63 L/kg 7808.94 ng·h/mL /
In Vivo

GPR68 antagonist 1 (10-30 mg/kg; i.p.; daily; 10 days) significantly alleviates DSS-induced IBD symptoms in C57BL/6 mice, including reduced weight loss, colonic shortening, and pro-inflammatory cytokine production, while improving survival and colon tissue histology[1].

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

Animal Model: C57BL/6 (6-8 weeks old; DSS-induced IBD model)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: i.p.; daily; 10 days (day 0 to day 9)
Result: Delayed weight loss in DSS-exposed mice, with weight recovery observed after switching to normal water.
Reduced colonic shortening.
Prolonged mouse survival.
Mitigated colon tissue damage as shown by H&E staining.
Reduced infiltration of S100A9-positive inflammatory cells in colon tissues.
Significantly decreased serum levels of pro-inflammatory cytokines IL-6, IL-1β, and TNF-α.
Significantly reduced mRNA expression of Il-6, Il-1β, and Tnf-α in colon tissues.
Molecular Weight

430.49

Formula

C28H24F2O2
SMILES

FC1=CC=C(CC(C2=CC=C(O)C=C2)C(C3=CC=C(O)C=C3)CC4=CC=C(F)C=C4)C=C1
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.

GPR68 antagonist 1 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:

GPR68 antagonist 1GPR68TNF ReceptorInterleukin RelatedG Protein-Coupled Receptor 68Tumor Necrosis Factor ReceptorTNFRILBEAS-2B cellsinflammatory bowel diseasecAMP signalingHEK293T cellsAC16 cellsHK-2 cellsdextran sulfate sodiumC57BL/6 micepro-inflammatory cytokinesInhibitorinhibitorinhibit

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:
GPR68 antagonist 1
Cat. No.:
HY-181485
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.