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Supplier NameMedChemExpress (MCE)
Contactsales
Tel609-228-6898
Mobile609-228-6898
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Emailsales@medchemexpress.com; tech@medchemexpress.com
Websitehttps://www.medchemexpress.com/
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Product NameSeripiprant
Synonyms KYTH105
KYTH 105
ACT129968
KYTH-105
ACT129968
ACT 129968
Setipiprant

Synonyms

KYTH105
KYTH 105
ACT129968
KYTH-105
ACT129968
ACT 129968
Setipiprant
Seripiprant
SETIPIPRANT
ACT-129968 (Setipiprant)
2-(2-(1-naphthoyl)-8-fluoro-1,2,3,4-tetrahydropyrido[4,3-b]indol-5-yl)acetic acid
2-(2-(1-Naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid
2-[8-fluoro-2-(naphthalene-1-carbonyl)-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
8-Fluoro-1,2,3,4-tetrahydro-2-(1-naphthalenylcarbonyl)-5H-pyrido[4,3-b]indole-5-acetic acid
CAS866460-33-5
EINECS
Chemical FormulaC24H19FN2O3
Molecular Weight402.42
inchi
Package10 mM * 1 mL;10 mM * 1 mL;5 mg;5 mg;10 mg;10 mg;25 mg;25 mg;50 mg;50 mg
PriceEmail to quote
DescriptionsSetipiprant

Setipiprant

MedChemExpress (MCE)

HY-16635

866460-33-5

ACT-129968

Descriptions

Setipiprant

Setipiprant

MedChemExpress (MCE)

HY-16635

866460-33-5

ACT-129968
KYTH-105

98.23%

Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Room temperature in continental US
may vary elsewhere.

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.

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].

1.19 Pharmacokinetic Properties of Setipiprant in Rats and Dogs[1]. AUC0-last (ng•h/mL) CL (mL/min/kg) T1/2 (hr) F (%) RatsIV 2 mg/kg 58500 1.3 6 44 DogsPO 10 mg/kg 91100 55

hCRTH2 6 nM (IC50) hDP1 1290 nM (IC50) EP2 2600 nM (IC50)

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[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.

Supplier Websitehttps://www.medchemexpress.com/Setipiprant.html
Last Update2025-05-21 16:50:25
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