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Purity: ≥98%
Fevipiprant (formerly known as NVP-QAW039 or QAW039) is a novel, selective, potent, oral active and reversible competitive CRTh2 (chemoattractant receptor-homologous molecules expressed on T-helper type 2) antagonist with an in vitro dissociation constant KD value of 1.1nM at the CRTh2 receptor and an IC50 value of 0.44 nM for inhibition of PGD2-induced eosinophil shape change in human whole blood. It is currently being developed to treat allergic diseases and may be used to treat asthma. The human CRTh2 receptor (1.14 ± 0.44 nM) expressed in Chinese hamster ovary cells was highly affinified for [(3)H]-QAW039, and the binding was both competitive and reversible with the native agonist prostaglandin D2 (PGD2).
| Targets |
DP2 ( Kd = 1.14 nM )
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| ln Vitro |
Fevipiprant (0-10 µM) inhibits the expression of the following genes in human Th2 cells stimulated by activated mast cell supernatants: IL-4, IL-3, IL-5, IL-8, CSF1, and CSF2[1].
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| ln Vivo |
Fevipiprant (10 mg/kg; in the drinking water) inhibits the formation of mouse abdominal aortic aneurysms (AAAs) induced by CaCl2[3].
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| Animal Protocol |
C57Bl/6 mice
10 mg/kg In the drinking water |
| References |
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| Molecular Formula |
C19H17F3N2O4S
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| Molecular Weight |
426.41
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| Exact Mass |
426.09
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| Elemental Analysis |
C, 53.52; H, 4.02; F, 13.37; N, 6.57; O, 15.01; S, 7.52
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| CAS # |
872365-14-5
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| Related CAS # |
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| Appearance |
White to off-white solid powder
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| SMILES |
CC1=C(C2=C(N1CC3=C(C=C(C=C3)S(=O)(=O)C)C(F)(F)F)N=CC=C2)CC(=O)O
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| InChi Key |
GFPPXZDRVCSVNR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17F3N2O4S/c1-11-15(9-17(25)26)14-4-3-7-23-18(14)24(11)10-12-5-6-13(29(2,27)28)8-16(12)19(20,21)22/h3-8H,9-10H2,1-2H3,(H,25,26)
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| Chemical Name |
2-[2-methyl-1-[[4-methylsulfonyl-2-(trifluoromethyl)phenyl]methyl]pyrrolo[2,3-b]pyridin-3-yl]acetic acid
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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: ≥ 2.5 mg/mL (5.86 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 25.0 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: ≥ 2.5 mg/mL (5.86 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 25.0 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: ≥ 2.5 mg/mL (5.86 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 | 2.3452 mL | 11.7258 mL | 23.4516 mL | |
| 5 mM | 0.4690 mL | 2.3452 mL | 4.6903 mL | |
| 10 mM | 0.2345 mL | 1.1726 mL | 2.3452 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 |
| NCT03665701 | Completed | Procedure: Blood Sampling | Atopic Asthma | Fraunhofer-Institute of Toxicology and Experimental Medicine |
August 16, 2018 | Not Applicable |
| NCT03087942 | Completed | Drug: QAW039 Drug: QAW39A |
Renal Insufficiency | Novartis Pharmaceuticals | July 5, 2017 | Phase 1 |
| NCT03681093 | Completed | Drug: Fevipiprant 150 mg Drug: Fevipiprant 450 mg |
Nasal Polyps | Novartis Pharmaceuticals | March 26, 2019 | Phase 3 |
| NCT03048448 | Completed | Drug: Fevipiprant | Hepatic Impairment | Novartis Pharmaceuticals | May 31, 2017 | Phase 1 |
| NCT03226392 | Completed | Drug: QAW039 Drug: Placebo |
Asthma | Novartis Pharmaceuticals | October 31, 2017 | Phase 3 |
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