WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 317129

CAS#: 866460-33-5

Description: Setipiprant, also known as ACT-129968 and KYTH-105, is a potent and selective CRTH2 antagonist. Setipiprant at multiple oral doses was well tolerated and reduced both the allergen-induced LAR and the associated AHR in allergic asthmatics. Our findings confirm that CRTH2 may be a promising target for the treatment of allergic disorders.

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Setipiprant, purity > 98%, is in stock. The same day shipping out after order is received.

Chemical Structure


Theoretical Analysis

MedKoo Cat#: 317129
Name: Setipiprant
CAS#: 866460-33-5
Chemical Formula: C24H19FN2O3
Exact Mass: 402.13797
Molecular Weight: 402.43
Elemental Analysis: C, 71.63; H, 4.76; F, 4.72; N, 6.96; O, 11.93

Synonym: ACT-129968; ACT 129968; ACT129968; KYTH-105; KYTH105; KYTH 105; Setipiprant

IUPAC/Chemical Name: 2-(2-(1-naphthoyl)-8-fluoro-1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indol-5-yl)acetic acid


InChi Code: InChI=1S/C24H19FN2O3/c25-16-8-9-21-19(12-16)20-13-26(11-10-22(20)27(21)14-23(28)29)24(30)18-7-3-5-15-4-1-2-6-17(15)18/h1-9,12H,10-11,13-14H2,(H,28,29)

SMILES Code: FC(C=C1)=CC2=C1N(CC(O)=O)C3=C2CN(C(C4=CC=CC5=CC=CC=C54)=O)CC3

Technical Data

Solid powder

>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:


1: Risch P, Pfeifer T, Segrestaa J, Fretz H, Pothier J. Verification of the Major Metabolic Oxidation Path for the Naphthoyl Group in Chemoattractant Receptor-Homologous Molecule Expressed on Th2 Cells (CRTh2) Antagonist 2-(2-(1-Naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic Acid (Setipiprant/ACT-129968). J Med Chem. 2015 Oct 2. [Epub ahead of print] PubMed PMID: 26398218.

2: Gehin M, Sidharta PN, Gnerre C, Treiber A, Halabi A, Dingemanse J. Pharmacokinetic interactions between simvastatin and setipiprant, a CRTH2 antagonist. Eur J Clin Pharmacol. 2015 Jan;71(1):15-23. doi: 10.1007/s00228-014-1767-x. Epub 2014 Oct 18. PubMed PMID: 25323804.

3: Diamant Z, Sidharta PN, Singh D, O'Connor BJ, Zuiker R, Leaker BR, Silkey M, Dingemanse J. Setipiprant, a selective CRTH2 antagonist, reduces allergen-induced airway responses in allergic asthmatics. Clin Exp Allergy. 2014 Aug;44(8):1044-52. doi: 10.1111/cea.12357. PubMed PMID: 24964348.

4: Sidharta PN, Diamant Z, Dingemanse J. Single- and multiple-dose tolerability and pharmacokinetics of the CRTH2 antagonist setipiprant in healthy male subjects. Fundam Clin Pharmacol. 2014 Dec;28(6):690-9. doi: 10.1111/fcp.12079. Epub 2014 May 11. PubMed PMID: 24734908.

5: Hoch M, Wank J, Kluge I, Wagner-Redeker W, Dingemanse J. Disposition and metabolism of setipiprant, a selective oral CRTH2 antagonist, in humans. Drugs R D. 2013 Dec;13(4):253-69. doi: 10.1007/s40268-013-0031-7. PubMed PMID: 24214422; PubMed Central PMCID: PMC3851755.

6: Baldoni D, Mackie A, Gutierrez M, Theodor R, Dingemanse J. Setipiprant, a selective oral antagonist of human CRTH2: relative bioavailability of a capsule and a tablet formulation in healthy female and male subjects. Clin Ther. 2013 Nov;35(11):1842-8. doi: 10.1016/j.clinthera.2013.09.003. Epub 2013 Oct 4. PubMed PMID: 24095247.

7: Norman P. Update on the status of DP2 receptor antagonists; from proof of concept through clinical failures to promising new drugs. Expert Opin Investig Drugs. 2014 Jan;23(1):55-66. doi: 10.1517/13543784.2013.839658. Epub 2013 Sep 27. Review. PubMed PMID: 24073896.

8: Fretz H, Valdenaire A, Pothier J, Hilpert K, Gnerre C, Peter O, Leroy X, Riederer MA. 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) antagonist. J Med Chem. 2013 Jun 27;56(12):4899-911. doi: 10.1021/jm400122f. Epub 2013 Jun 13. PubMed PMID: 23721423.