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Purity: ≥98%
Grapiprant (formerly known as CJ-023,423, RQ-00000007, or AAT-007) is a selective and potent EP4 receptor antagonist. It might possess antihyperalgesic qualities. With K(i) of 13 +/- 4 and 20 +/- 1 nM, respectively, CJ-023,423 inhibits [(3)H]-labeled PGE(2) binding to both human and rat EP(4) receptors in vitro. Human EP(4) receptors are highly selective for CJ-023,423 compared to other human prostanoid receptor subtypes. Additionally, it suppresses the increase in intracellular cAMP induced by PGE(2) at the rat and human EP(4) receptors, where pA(2) is 8.2 +/- 0.2 nM and 8.3 +/- 0.03 nM, respectively. Oral CJ-023,423 administration dramatically lessens the thermal hyperalgesia brought on by intraplantar PGE(2) injection (ED(50) = 12.8 mg/kg) in vivo.
| Targets |
human EP4 receptor ( Ki = 13 nM ); rat EP4 receptor ( Ki = 20 nM ); EP4 ( Ki = 24 nM ); EP4 ( IC50 = 35 nM )
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| ln Vivo |
Grapiprant (0-50 mg/kg; oral administration; every 24 hours; for 9 months; beagles) is safe to give orally to dogs on a long-term basis. Further research is required to determine whether Grapiprant is effective in treating dogs with osteoarthritis[3].
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| Animal Protocol |
36 beagles of both sexes (9-month-old)
0 mg/kg, 1 mg/kg, 6 mg/kg, or 50 mg/kg Oral administration; every 24 hours; for 9 months |
| References |
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| Molecular Formula |
C26H29N5O3S
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| Molecular Weight |
491.61
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| Exact Mass |
491.2
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| Elemental Analysis |
C, 63.52; H, 5.95; N, 14.25; O, 9.76; S, 6.52
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| CAS # |
415903-37-6
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| Related CAS # |
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| Appearance |
Solid powder
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| 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
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| InChi Key |
HZVLFTCYCLXTGV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H29N5O3S/c1-5-24-29-25-19(4)28-18(3)16-23(25)31(24)21-10-8-20(9-11-21)14-15-27-26(32)30-35(33,34)22-12-6-17(2)7-13-22/h6-13,16H,5,14-15H2,1-4H3,(H2,27,30,32)
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| Chemical Name |
1-[2-[4-(2-ethyl-4,6-dimethylimidazo[4,5-c]pyridin-1-yl)phenyl]ethyl]-3-(4-methylphenyl)sulfonylurea
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (6.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (6.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3 mg/mL (6.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05041101 | Active Recruiting |
Drug: Eribulin Mesylate Drug: Grapiprant |
Breast Inflammatory Carcinoma Recurrent Breast Inflammatory Carcinoma |
M.D. Anderson Cancer Center | November 4, 2021 | Phase 1 Phase 2 |
| NCT03658772 | Completed | Drug: grapiprant Drug: grapiprant and pembrolizumab |
Microsatellite Stable Colorectal Cancer |
Arrys Therapeutics | September 20, 2018 | Phase 1 |
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