Setipiprant

Modify Date: 2024-01-02 19:28:38

Setipiprant Structure
Setipiprant structure
Common Name Setipiprant
CAS Number 866460-33-5 Molecular Weight 402.418
Density 1.4±0.1 g/cm3 Boiling Point 690.4±55.0 °C at 760 mmHg
Molecular Formula C24H19FN2O3 Melting Point N/A
MSDS N/A Flash Point 371.4±31.5 °C

 Use of Setipiprant


Setipiprant is an orally available, selective CRTH2 antagonist. CRTH2 is a G protein-coupled receptor for PGD2.IC50 value: 6.0 nMTarget: PGD2in vitro: Setipiprant is an orally available, selective CRTH2 (chemoattractant receptor-homologous molecule expressed on T helper [Th]-2 cells) antagonist. CRTH2 is a G protein-coupled receptor for prostaglandin (PGD2). PGD2 is produced by the mast cells and is a key mediator in various inflammatory diseases, including allergy and asthma. Binding of PGD2 to CRTH2, which are expressed on the surface of blood-borne cells, induces chemotaxis of Th2 cells, basophils, and eosinophils, and stimulates cytokine release from these cells. Thus, antagonism of CRTH2 receptors is considered to be a promising therapeutic target for various allergic diseases and asthma.

 Names

Name 2-[8-fluoro-2-(naphthalene-1-carbonyl)-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
Synonym More Synonyms

 Setipiprant Biological Activity

Description Setipiprant is an orally available, selective CRTH2 antagonist. CRTH2 is a G protein-coupled receptor for PGD2.IC50 value: 6.0 nMTarget: PGD2in vitro: Setipiprant is an orally available, selective CRTH2 (chemoattractant receptor-homologous molecule expressed on T helper [Th]-2 cells) antagonist. CRTH2 is a G protein-coupled receptor for prostaglandin (PGD2). PGD2 is produced by the mast cells and is a key mediator in various inflammatory diseases, including allergy and asthma. Binding of PGD2 to CRTH2, which are expressed on the surface of blood-borne cells, induces chemotaxis of Th2 cells, basophils, and eosinophils, and stimulates cytokine release from these cells. Thus, antagonism of CRTH2 receptors is considered to be a promising therapeutic target for various allergic diseases and asthma.
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 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 690.4±55.0 °C at 760 mmHg
Molecular Formula C24H19FN2O3
Molecular Weight 402.418
Flash Point 371.4±31.5 °C
Exact Mass 402.137970
PSA 62.54000
LogP 3.39
Vapour Pressure 0.0±2.3 mmHg at 25°C
Index of Refraction 1.682
Storage condition -20℃

 Synonyms

[8-Fluoro-2-(1-naphthoyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indol-5-yl]acetic acid
Setipiprant
5H-Pyrido[4,3-b]indole-5-acetic acid, 8-fluoro-1,2,3,4-tetrahydro-2-(1-naphthalenylcarbonyl)-
UNII-BHF20LA2GM
2-(2-(1-Naphthoyl)-8-fluoro-1,2,3,4-tetrahydropyrido[4,3-b]indol-5-yl)acetic acid
ACT-129968
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