1. GPCR/G Protein
  2. Prostaglandin Receptor

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

Cat. No.: HY-16635 Purity: 98.14%
Data Sheet SDS Handling Instructions

Setipiprant is an orally available, selective CRTH2 antagonist. CRTH2 is a G protein-coupled receptor for PGD2.

For research use only. We do not sell to patients.
Setipiprant Chemical Structure

Setipiprant Chemical Structure

CAS No. : 866460-33-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $143 In-stock
5 mg $130 In-stock
10 mg $210 In-stock
50 mg $650 In-stock
100 mg $950 In-stock
200 mg $1500 In-stock
500 mg $3000 In-stock
1 g   Get quote  
5 g   Get quote  

* Please select Quantity before adding items.

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

Description

Setipiprant is an orally available, selective CRTH2 antagonist. CRTH2 is a G protein-coupled receptor for PGD2. IC50 value: 6.0 nM Target: PGD2 in 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.

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01877629 Actelion Healthy June 2011 Phase 1
NCT01241214 Actelion Seasonal Allergic Rhinitis November 2010 Phase 2
NCT01225315 Actelion Asthma October 2010 Phase 2
NCT01484119 Actelion Seasonal Allergic Rhinitis December 2011 Phase 3
NCT01877629 Actelion Healthy June 2011 Phase 1
NCT01241214 Actelion Seasonal Allergic Rhinitis November 2010 Phase 2
NCT01225315 Actelion Asthma October 2010 Phase 2
NCT01484119 Actelion Seasonal Allergic Rhinitis December 2011 Phase 3
NCT02781311 Allergan Alopecia June 29, 2016 Phase 2
NCT02381496 Actelion Healthy December 2011 Phase 1
View MoreCollapse
Preparing Stock Solutions
Concentration Volume (DMSO) 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
Molecular Weight

402.42

Formula

C₂₄H₁₉FN₂O₃

CAS No.

866460-33-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 36 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Setipiprant
Cat. No.:
HY-16635
Quantity: