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

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

Cat. No.: HY-16781 Purity: 99.57%
COA 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 has the potential for osteoarthritic pain and inflammation treatment[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
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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 has the potential for osteoarthritic pain and inflammation treatment[1][2][3] .

IC50 & Target[2]

dog EP4

35 nM (IC50)

dog EP4

24 nM (Ki)

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] .

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

Appearance

Solid

Formula

C26H29N5O3S
CAS No.
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 2 years
-20°C 1 year
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 available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.57%

COA (248 KB) HNMR (267 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References
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Grapiprant Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

Grapiprant415903-37-6CJ-023423 RQ-00000007 AAT-007CJ023423CJ 023423RQ00000007RQ 00000007RQ-00000007AAT007AAT 007AAT-007Prostaglandin ReceptorInhibitorinhibitorinhibit

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