1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. Grapiprant

Grapiprant (Synonyms: CJ-023423; RQ-00000007; AAT-007)

Cat. No.: HY-16781 Purity: 99.68%
Handling Instructions

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 can be used to treat osteoarthritic pain and inflammation in healthy dogs[3] .

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

Grapiprant Chemical Structure

Grapiprant Chemical Structure

CAS No. : 415903-37-6

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10 mM * 1 mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 180 In-stock
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50 mg USD 550 In-stock
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Based on 3 publication(s) in Google Scholar

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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 can be used to treat osteoarthritic pain and inflammation in healthy dogs[1][2][3] .

IC50 & Target[2]

EP4

35 nM (IC50)

In Vivo

Grapiprant (0-50 mg/kg; oral administration; every 24 hours; for 9 months; beagles) is safe for dogs by long-term oral administration. Efficacy of Grapiprant in the treatment of dogs with osteoarthritis needs to be evaluated in other studies[3] .

Animal Model: 36 beagles of both sexes (9-month-old)[3]
Dosage: 0 mg/kg, 1 mg/kg, 6 mg/kg, or 50 mg/kg
Administration: Oral administration; every 24 hours; for 9 months
Result: Long-term oral administration was safe for dogs.
Clinical Trial
Molecular Weight

491.61

Formula

C₂₆H₂₉N₅O₃S

CAS No.

415903-37-6

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (101.71 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0341 mL 10.1707 mL 20.3413 mL
5 mM 0.4068 mL 2.0341 mL 4.0683 mL
10 mM 0.2034 mL 1.0171 mL 2.0341 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3 mg/mL (6.10 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 3 mg/mL (6.10 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 3 mg/mL (6.10 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.68%

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Grapiprant
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HY-16781
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