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Grapiprant

CAT: 0804-HY-16781-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-16781-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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] .
CAS Number
415903-37-6
Product Name Alternative
CJ-023423; RQ-00000007; AAT-007
UNSPSC
12352005
Hazard Statement
H302
Target
Prostaglandin Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein
Applications
Metabolism-protein/nucleotide metabolism
Field of Research
Metabolic Disease; Endocrinology; Cancer
Assay Protocol
https://www.medchemexpress.com/Grapiprant.html
Purity
99.57
Solubility
DMSO : ≥ 50 mg/mL
Smiles
O=S(C1=CC=C(C)C=C1)(NC(NCCC2=CC=C(N3C(CC)=NC4=C3C=C(C)N=C4C)C=C2)=O)=O
Molecular Formula
C26H29N5O3S
Molecular Weight
491.61
Precautions
H302
References & Citations
[1]Vito VD, et al. Detection and quantification of the selective EP4 receptor antagonist CJ-023423 (grapiprant) in canine plasma by HPLC with spectrofluorimetric detection. J Pharm Biomed Anal. 2016 Jan 25;118:251-8.|[2]Nagahisa A, et al. Pharmacology of grapiprant, a novel EP4 antagonist: receptor binding, efficacy in a rodent postoperative pain model, and a dose estimation for controlling pain in dogs. J Vet Pharmacol Ther. 2017 Jun;40 (3) :285-292.|[3]Rausch-Derra LC, et al. Evaluation of the safety of long-term, daily oral administration of grapiprant, a novel drug for treatment of osteoarthritic pain and inflammation, in healthy dogs.Am J Vet Res. 2015 Oct;76 (10) :853-9.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
EP

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