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Chemical Structure| 415903-37-6 Chemical Structure| 415903-37-6

Structure of Grapiprant
CAS No.: 415903-37-6

Chemical Structure| 415903-37-6

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Grapiprant is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2).

Synonyms: CJ-023423; RQ-00000007; CAS#415903-37-6

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Product Details of Grapiprant

CAS No. :415903-37-6
Formula : C26H29N5O3S
M.W : 491.61
SMILES Code : O=S(C1=CC=C(C)C=C1)(NC(NCCC2=CC=C(N3C(CC)=NC4=C3C=C(C)N=C4C)C=C2)=O)=O
Synonyms :
CJ-023423; RQ-00000007; CAS#415903-37-6
MDL No. :MFCD16628076
InChI Key :HZVLFTCYCLXTGV-UHFFFAOYSA-N
Pubchem ID :11677589

Safety of Grapiprant

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H319
Precautionary Statements:P264-P270-P280-P301+P312+P330-P305+P351+P338-P337+P313-P501

Related Pathways of Grapiprant

GPCR

Isoform Comparison

Biological Activity

Description
Grapiprant (CJ-023423) is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2). Grapiprant displaces [3H]-PGE2 (1 nM) binding to dog recombinant EP4 receptor with IC50 value of 35 nM and Ki value of 24 nM. Grapiprant has the potential for osteoarthritic pain and inflammation treatment[1].[2].[3].

In Vitro:

Cell Line
Concentration Treated Time Description References
neonatal rat cardiomyocytes (NRCMs) 1 μM 30 minutes To investigate the effect of grapiprant on ISO-induced TGF-β1 secretion, results showed grapiprant effectively inhibited ISO-induced TGF-β1 secretion. Adv Sci (Weinh). 2025 Mar;12(12):e2413324

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD mice Prediabetic model Oral 10 mg/kg body weight Once daily for 4 weeks Inhibition of PTGER4 signaling restored IFNAR signaling, decreased IL-1 signaling, and reduced leukocyte infiltration into the islets. JCI Insight. 2018 Feb 8;3(3):e97843
Dogs Acute arthritis model Oral 1.5 to 2.9 mg/kg Single dose To evaluate the analgesic efficacy of grapiprant in an acute arthritis model, results showed no significant difference compared to untreated controls BMC Vet Res. 2019 Aug 29;15(1):309
Dogs Young dogs with appendicular joint osteoarthritis pain model Oral 2 mg/kg Once daily for 4 months To evaluate the efficacy of Grapiprant as part of a multimodal treatment regimen for osteoarthritis pain in young dogs. Results showed significant improvement in pain scores and limb use. Front Vet Sci. 2024 Oct 24;11:1461628

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT04365699 COVID-19 PHASE2 COMPLETED 2021-01-31 NYU Langone Health, New York, ... More >>New York, 10016, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.17mL

2.03mL

1.02mL

20.34mL

4.07mL

2.03mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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