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GPR4 antagonist 3 

Cat. No.: HY-101784
Handling Instructions

GPR4 antagonist 3 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. Anti-inflammatory activities.

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

GPR4 antagonist 3 Chemical Structure

GPR4 antagonist 3 Chemical Structure

CAS No. : 1401728-56-0

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Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References


GPR4 antagonist 3 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM[1]. Anti-inflammatory activities[1].

IC50 & Target

IC50: 70 nM (GPR4)[1].

In Vivo

GPR4 antagonist 3 (compound 13) shows a significant anti-inflammatory effect in the rat antigen induced arthritis model after oral administration at 30 mg/kg bid for 20 days[1]. GPR4 antagonist 3 (30 mg/kg bid po for 4 days) also prevents angiogenesis in the mouse chamber model as well as pain as demonstrated in the rat complete Freund’s adjuvant model[1].

Animal Model: Female FVB mice (8−10 weeks)[1]
Dosage: 30 mg/kg bid po
Administration: Oral, 4 days, bid
Result: Treatment with GPR4 antagonist 3 at 30 mg/ kg po bid starting on day 0, the day of the chamber implantation, showS a statistically significant reduction (46.8 ± 10.6%) of tissue growth by day 4. The blood levels of 13 on day 4 at 2 and 16 h after compound application in this model are 9.03 ± 2.87 and 0.09 ± 0.06 μM[1].
Animal Model: Male Wistar Han rats[1]
Dosage: 3, 10, and 30 mg/kg
Administration: Oral, 20 days, bid
Result: GPR4 antagonist 3 displays not only higher exposures in the rat AIA but also lower plasma protein binding in rat (95%)[1].
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4008 mL 12.0042 mL 24.0085 mL
5 mM 0.4802 mL 2.4008 mL 4.8017 mL
10 mM 0.2401 mL 1.2004 mL 2.4008 mL
*Please refer to the solubility information to select the appropriate solvent.
Molecular Weight









Please store the product under the recommended conditions in the Certificate of Analysis.


Room temperature in continental US; may vary elsewhere

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Product Name:
GPR4 antagonist 3
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GPR4 antagonist 3

Cat. No.: HY-101784