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Grapiprant

Catalog No. TQ0292 CAS 415903-37-6

Synonyms: AAT-007, RQ-00000007, CJ-023423

Grapiprant (AAT-007) is a selective EP4 receptor antagonist. Grapiprant displaces [3H]-PGE2 (1 nM) binding to dog recombinant EP4 receptor (IC50: 35 nM, Ki: 24 nM).

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Grapiprant, CAS 415903-37-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
2 mg	In stock	$ 44.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 197.00
50 mg	In stock	$ 372.00
100 mg	In stock	$ 562.00
200 mg	In stock	$ 849.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 99.49%

Biological Description

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Description	Grapiprant (AAT-007) is a selective EP4 receptor antagonist. Grapiprant displaces [3H]-PGE2 (1 nM) binding to dog recombinant EP4 receptor (IC50: 35 nM, Ki: 24 nM).
Targets&IC50	EP4:35 nM
In vivo	Grapiprant (0-50 mg/kg; p.o; every 24 hours; for 9 months; beagles) is safe for dogs by long-term oral administration [2].
Animal Research	Animal Model: 36 beagles of both sexes (9-month-old). Dosage: 0 mg/kg, 1 mg/kg, 6 mg/kg, or 50 mg/kg. Administration: Oral administration; every 24 hours; for 9 months [2]

Synonyms	AAT-007, RQ-00000007, CJ-023423
Molecular Weight	491.61
Formula	C26H29N5O3S
CAS No.	415903-37-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 48 mg/mL (97.64 mM)

References and Literature

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. 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. 3. 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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Inhibitor Library GPCR Compound Library Anti-Cancer Drug Library Anti-Lung Cancer Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max Anti-Prostate Cancer Compound Library

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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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Grapiprant 415903-37-6 GPCR/G Protein Immunology/Inflammation Prostaglandin Receptor AAT 007 AAT007 Inhibitor AAT-007 CJ 023423 RQ 00000007 RQ-00000007 CJ023423 inhibit RQ00000007 CJ-023423 inhibitor

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