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Setipiprant (ACT-129968) is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). CRTH2, a G protein-coupled receptor for prostaglandin (PGD2), mediates key inflammatory responses related to allergy and asthma. PGD2, produced by mast cells, binds to CRTH2 on blood-borne cells, inducing chemotaxis of Th2 cells, basophils, and eosinophils, and stimulating cytokine release.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | $39 | In Stock | In Stock | |
| 25 mg | $72 | In Stock | In Stock | |
| 50 mg | $118 | In Stock | In Stock | |
| 100 mg | $189 | In Stock | In Stock | |
| 200 mg | $278 | In Stock | - | |
| 1 mL x 10 mM (in DMSO) | $30 | In Stock | In Stock |
| Description | Setipiprant (ACT-129968) is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). CRTH2, a G protein-coupled receptor for prostaglandin (PGD2), mediates key inflammatory responses related to allergy and asthma. PGD2, produced by mast cells, binds to CRTH2 on blood-borne cells, inducing chemotaxis of Th2 cells, basophils, and eosinophils, and stimulating cytokine release. |
| Targets&IC50 | CRTH2:6.0 nM, DP1 (human):1290 nM, EP2:2600 nM |
| Synonyms | KYTH-105, ACT-129968 |
| Molecular Weight | 402.42 |
| Formula | C24H19FN2O3 |
| Cas No. | 866460-33-5 |
| Smiles | C(C(O)=O)N1C2=C(C=3C1=CC=C(F)C3)CN(C(=O)C=4C5=C(C=CC4)C=CC=C5)CC2 |
| Relative Density. | 1.37 g/cm3 (Predicted) |
| Color | White |
| Appearance | solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 45 mg/mL (111.82 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.97 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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