Setipiprant (Synonyms: ACT-129968; KYTH-105)

Cat. No.: HY-16635 Purity: 98.23%: FAQs
Data Sheet SDS COA Handling Instructions

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Setipiprant (ACT-129968) is an orally active and selective CRTH2 antagonist. Setipiprant interacts with hCRTH2 receptor with an IC₅₀ value of 6 nM. Setipiprant inhibits prostanoid receptors hDP₁ and hEP₂ with IC₅₀ values of 1290 and 2600 nM, respectively. Setipiprant can be used for the research of asthma and rhinitis.

For research use only. We do not sell to patients.

Setipiprant Chemical Structure

CAS No. : 866460-33-5

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10 mM * 1 mL in DMSO ready for reconstitution	USD 39	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 39	In-stock	Estimated Time of Arrival: December 31
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25 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

hCRTH2

6 nM (IC₅₀)

hDP1

1290 nM (IC₅₀)

EP2

2600 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	1290 nM Compound: 28, Setipiprant, ACT-129968	Displacement of [3H]PGD2 from recombinant human prostanoid DP1 receptor expressed in CHO cells after 90 mins by scintillation counting analysis Displacement of [3H]PGD2 from recombinant human prostanoid DP1 receptor expressed in CHO cells after 90 mins by scintillation counting analysis	[PMID: 23721423]
CHO-K1	IC₅₀	> 25 μM Compound: 28, Setipiprant, ACT-129968	Antagonist activity at human prostanoid EP1 receptor expressed in CHOK1 cells assessed as inhibition of PGE2-induced calcium flux after 60 mins by FLIPR assay Antagonist activity at human prostanoid EP1 receptor expressed in CHOK1 cells assessed as inhibition of PGE2-induced calcium flux after 60 mins by FLIPR assay	[PMID: 23721423]
HEK293	IC₅₀	> 10 μM Compound: 28, Setipiprant, ACT-129968	Displacement of [3H]PGE2 from recombinant human prostanoid EP4 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting analysis Displacement of [3H]PGE2 from recombinant human prostanoid EP4 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting analysis	[PMID: 23721423]
HEK293	IC₅₀	> 10000 nM Compound: 28, Setipiprant, ACT-129968	Inhibition of beta-arrestin binding to recombinant human prostanoid EP4 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay Inhibition of beta-arrestin binding to recombinant human prostanoid EP4 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay	[PMID: 23721423]
HEK293	IC₅₀	> 25 μM Compound: 28, Setipiprant, ACT-129968	Antagonist activity at human prostanoid TP2 receptor expressed in HEK293 cells assessed as inhibition of calcium flux after 30 to 40 mins by FLIPR assay Antagonist activity at human prostanoid TP2 receptor expressed in HEK293 cells assessed as inhibition of calcium flux after 30 to 40 mins by FLIPR assay	[PMID: 23721423]
HEK293	IC₅₀	> 25 μM Compound: 28, Setipiprant, ACT-129968	Antagonist activity at human prostanoid EP3 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced calcium flux after 60 mins by FLIPR assay Antagonist activity at human prostanoid EP3 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced calcium flux after 60 mins by FLIPR assay	[PMID: 23721423]
HEK293	IC₅₀	2600 nM Compound: 28, Setipiprant, ACT-129968	Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay	[PMID: 23721423]
HEK293	IC₅₀	30 nM Compound: 28, Setipiprant, ACT-129968	Antagonist activity at human CRTH2 receptor expressed in HEK293 cells assessed as inhibition of PGD2-induced calcium flux after 5 mins by FLIPR assay Antagonist activity at human CRTH2 receptor expressed in HEK293 cells assessed as inhibition of PGD2-induced calcium flux after 5 mins by FLIPR assay	[PMID: 23721423]
HEK293	IC₅₀	340 nM Compound: 28, Setipiprant, ACT-129968	Displacement of [3H]PGD2 from recombinant human CRTH2 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting analysis in presence of human serum albumin Displacement of [3H]PGD2 from recombinant human CRTH2 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting analysis in presence of human serum albumin	[PMID: 23721423]
HEK293	IC₅₀	6 nM Compound: 28, Setipiprant, ACT-129968	Displacement of [3H]PGD2 from recombinant human CRTH2 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting analysis Displacement of [3H]PGD2 from recombinant human CRTH2 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting analysis	[PMID: 23721423]
HEK293	IC₅₀	80 nM Compound: 28, Setipiprant, ACT-129968	Antagonist activity at human CRTH2 receptor expressed in HEK293 cells assessed as inhibition of PGD2/forskolin-induced intracellular cAMP production after 20 mins by ELISA Antagonist activity at human CRTH2 receptor expressed in HEK293 cells assessed as inhibition of PGD2/forskolin-induced intracellular cAMP production after 20 mins by ELISA	[PMID: 23721423]

In Vitro

Setipiprant (0-10 μM; 90 min) interacts with hCRTH2 receptor in the absence and presence of Human Serum Albumin (HSA) in the assay buffer with IC₅₀ values of 6 and 340 nM, respectively^[1].
Setipiprant (0-10 μM; 5-20 min) inhibits hCRTH2 receptor based intracellular calcium liberation, intracellular cAMP and shape change of human eosinophils with IC₅₀ values of 30, 80 and 235 nM, respectively^[1].
Setipiprant (0-10 μM) inhibits prostanoid receptors hDP₁, hEP₂ and hEP₄ with IC₅₀ values of 1290, 2600 and ＞10000 nM, respectively^[1].

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

In Vivo

1.19 Pharmacokinetic Properties of Setipiprant in Rats and Dogs^[1].

	AUC_0-last (ng•h/mL)	CL (mL/min/kg)	T_1/2 (hr)	F (%)
Rats IV 2 mg/kg	58500	1.3	6	44
Dogs PO 10 mg/kg	91100			55

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

Clinical Trial

Molecular Weight

402.42

Formula

C₂₄H₁₉FN₂O₃

CAS No.

866460-33-5

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(O)CN1C2=C(CN(C(C3=C4C=CC=CC4=CC=C3)=O)CC2)C5=C1C=CC(F)=C5

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 : ≥ 36 mg/mL (89.46 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4850 mL	12.4248 mL	24.8497 mL
5 mM	0.4970 mL	2.4850 mL	4.9699 mL
10 mM	0.2485 mL	1.2425 mL	2.4850 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.23%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (257 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[1]. Heinz Fretz, et al. Identification of 2 (2-(1-Naphthoyl)-8-fluoro-3,4-dihydro 1H pyrido[4,3 b]indol-5(2H) yl)acetic Acid (Setipiprant/ACT 129968), a Potent, Selective, and Orally Bioavailable Chemoattractant Receptor-Homologous Molecule Expressed on Th2 Cells (CRTH2) Antagonis. 2013.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4850 mL	12.4248 mL	24.8497 mL	62.1241 mL
	5 mM	0.4970 mL	2.4850 mL	4.9699 mL	12.4248 mL
	10 mM	0.2485 mL	1.2425 mL	2.4850 mL	6.2124 mL
	15 mM	0.1657 mL	0.8283 mL	1.6566 mL	4.1416 mL
	20 mM	0.1242 mL	0.6212 mL	1.2425 mL	3.1062 mL
	25 mM	0.0994 mL	0.4970 mL	0.9940 mL	2.4850 mL
	30 mM	0.0828 mL	0.4142 mL	0.8283 mL	2.0708 mL
	40 mM	0.0621 mL	0.3106 mL	0.6212 mL	1.5531 mL
	50 mM	0.0497 mL	0.2485 mL	0.4970 mL	1.2425 mL
	60 mM	0.0414 mL	0.2071 mL	0.4142 mL	1.0354 mL
	80 mM	0.0311 mL	0.1553 mL	0.3106 mL	0.7766 mL

Setipiprant Related Classifications

Inflammation/Immunology Endocrinology

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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