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Setipiprant

Name: Setipiprant
Brand: TargetMol
SKU: T3520
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3520Cas No. 866460-33-5

Alias KYTH-105, ACT-129968

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.

Setipiprant

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Purity: 99.16%

Catalog No. T3520Alias KYTH-105, ACT-129968Cas No. 866460-33-5

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$30	In Stock	In Stock
25 mg	$48	In Stock	In Stock
50 mg	$77	In Stock	In Stock
100 mg	$123	In Stock	In Stock
200 mg	$198	In Stock	-
1 mL x 10 mM (in DMSO)	$30	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.16%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Setipiprant AI Summary

Setipiprant exhibits prolonged elimination half-life in human and rat plasma, along with a favorable volume of distribution in Wistar rats. It demonstrates potent antagonist activity at the CRTH2 receptor with high selectivity over the DP1 receptor and significant protein binding in plasma. The compound shows promising oral bioavailability in both beagle dogs and Wistar rats, potent inhibition of CYP enzymes, various antagonist activities at different prostanoid receptors, and strong affinity for the CRTH2 receptor with a low IC50 value. Additionally, it has moderate intrinsic clearance in liver microsomes and hepatocytes, and satisfactory clearance rates in beagle dogs and Wistar rats. Furthermore, Setipiprant exhibits antiviral activity against SARS-CoV-2. It inhibits SARS-CoV-2 induced cytotoxicity of Caco-2 cells by 8.44% at a 10 µM concentration after 48 hours, and shows a slight inhibitory effect (-0.12%) on the cytotoxicity of VERO-6 cells under similar conditions. It also demonstrates inhibition of the SARS-CoV-2 3CL-Pro protease, with an observed effect of -7.312% at a 20 µM concentration. Despite these activities, the compound shows moderate potency (IC50 > 20,000 nM) in inhibiting virus-induced cytotoxic effects in VERO-6 cells. Setipiprant also shows inhibitory activity on the human HDAC6 enzyme, with 34.49% inhibition in an enzymatic assay using a commercial peptide substrate, though it showed -7.96% inhibition with a custom peptide substrate, suggesting a varied interaction dependent on the substrate used..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

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	DP1 (human):1290 nM, CRTH2:6.0 nM, EP2:2600 nM
Synonyms	KYTH-105, ACT-129968

Chemical Properties

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)

Storage & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	2.4850 mL	12.4248 mL	24.8497 mL	124.2483 mL
5 mM	0.4970 mL	2.4850 mL	4.9699 mL	24.8497 mL
10 mM	0.2485 mL	1.2425 mL	2.4850 mL	12.4248 mL
20 mM	0.1242 mL	0.6212 mL	1.2425 mL	6.2124 mL
50 mM	0.0497 mL	0.2485 mL	0.4970 mL	2.4850 mL
100 mM	0.0248 mL	0.1242 mL	0.2485 mL	1.2425 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc