Home GPCR & G Protein Prostaglandin Receptor antagonist Grapiprant (CJ-023,423) For research use only.

Grapiprant (CJ-023,423)

Synonyms: AT-001, AAT-007, RQ-00000007, CJ-23423

Grapiprant (CJ-023,423, AT-001, AAT-007, RQ-00000007, CJ-23423) is a novel selective EP4 Prostaglandin Receptor inhibitor with Ki of 20 nM and 13 nM for rat EP4 receptor and human EP4 receptor, respectively.

Grapiprant (CJ-023,423) Chemical Structure

Grapiprant (CJ-023,423) Chemical Structure

CAS: 415903-37-6

Selleck's Grapiprant (CJ-023,423) has been cited by 1 publication

Purity & Quality Control

Batch: S669401 DMSO] 98 mg/mL] false] Ethanol] 24 mg/mL] false] Water] Insoluble] false Purity: 99.6%
99.6

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Biological Activity

Description Grapiprant (CJ-023,423, AT-001, AAT-007, RQ-00000007, CJ-23423) is a novel selective EP4 Prostaglandin Receptor inhibitor with Ki of 20 nM and 13 nM for rat EP4 receptor and human EP4 receptor, respectively.
Targets
human EP4 receptor [1] rat EP4 receptor [1] EP4 [1]
(Cell-free assay)		 EP4 [1]
(Cell-free assay)
13 nM(Ki) 20 nM(Ki) 24 nM(Ki) 35 nM
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03696212 Terminated
Non-small Cell Lung Cancer Adenocarcinoma
Arrys Therapeutics|Merck Sharp & Dohme LLC
 January 8 2019 Phase 1|Phase 2
NCT03658772 Completed
Microsatellite Stable Colorectal Cancer
Arrys Therapeutics|Merck Sharp & Dohme LLC
 September 20 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 491.61 Formula

C26H29N5O3S
CAS No. 415903-37-6 SDF --
Smiles CCC1=NC2=C(N1C3=CC=C(C=C3)CCNC(=O)NS(=O)(=O)C4=CC=C(C=C4)C)C=C(N=C2C)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 98 mg/mL ( (199.34 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 24 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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