Asapiprant
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MedKoo CAT#: 319665

CAS#: 932372-01-5

Description: Asapiprant, also known as S-555739, is a the potent and selective DP1 receptor antagonist. Asapiprant exhibited high affinity and selectivity for the DP1 receptor. Significant suppression of antigen-induced nasal resistance, nasal secretion, and cell infiltration in nasal mucosa was observed with asapiprant treatment. In addition, treatment with asapiprant suppressed antigen-induced asthmatic responses, airway hyper-responsiveness, and cell infiltration and mucin production in lung. These results show that asapiprant is a potent and selective DP1 receptor antagonist, and exerts suppressive effects in the animal models of allergic diseases. Thus, asapiprant has potential as a novel therapy for allergic airway diseases.

Chemical Structure

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Asapiprant
CAS# 932372-01-5
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 319665
Name: Asapiprant
CAS#: 932372-01-5
Chemical Formula: C24H27N3O7S
Exact Mass: 501.16
Molecular Weight: 501.554
Elemental Analysis: C, 57.47; H, 5.43; N, 8.38; O, 22.33; S, 6.39

Price and Availability

Size Price Availability Quantity
10mg USD 150 Ready to ship
25mg USD 350 Ready to ship
50mg USD 550 Ready to ship
100mg USD 950 Ready to ship
200mg USD 1550 Ready to ship
500mg USD 2650 Ready to ship
1g USD 3950 Ready to ship
2g USD 6650 Ready to ship
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Synonym: S-555739; S 555739; S555739; Asapiprant

IUPAC/Chemical Name: 2-(5-(4-((4-isopropoxyphenyl)sulfonyl)piperazin-1-yl)-2-(oxazol-2-yl)phenoxy)acetic acid

InChi Key: ZMZNWNTZRWXTJU-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H27N3O7S/c1-17(2)34-19-4-6-20(7-5-19)35(30,31)27-12-10-26(11-13-27)18-3-8-21(24-25-9-14-32-24)22(15-18)33-16-23(28)29/h3-9,14-15,17H,10-13,16H2,1-2H3,(H,28,29)

SMILES Code: O=C(O)COC1=CC(N2CCN(S(=O)(C3=CC=C(OC(C)C)C=C3)=O)CC2)=CC=C1C4=NC=CO4

Appearance: Solid powder

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

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).

Solubility: 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).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: Asapiprant is a DP1 receptor antagonist with a Ki of 0.44 nM.
In vitro activity: TBD
In vivo activity: In the animal models of allergic rhinitis, changes in nasal resistance, nasal secretion, and cell infiltration in nasal mucosa were assessed after antigen challenge with and without asapiprant. Similarly, in the animal models of asthma, the effect of antigen challenge with and without asapiprant on antigen-induced bronchoconstriction, airway hyper-responsiveness, mucin production, and cell infiltration in lung were assessed. Significant suppression of antigen-induced nasal resistance, nasal secretion, and cell infiltration in nasal mucosa was observed with asapiprant treatment. In addition, treatment with asapiprant suppressed antigen-induced asthmatic responses, airway hyper-responsiveness, and cell infiltration and mucin production in lung. These results show that asapiprant exerts suppressive effects in the animal models of allergic diseases. Reference: Eur J Pharmacol. 2015 Oct 15;765:15-23. https://www.sciencedirect.com/science/article/abs/pii/S0014299915301795?via%3Dihub

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 7.1 14.08
DMF 10.0 19.94
DMF:PBS (pH 7.2) (1:5) 0.2 0.32

Preparing Stock Solutions

The following data is based on the product molecular weight 501.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Takahashi G, Asanuma F, Suzuki N, Hattori M, Sakamoto S, Kugimiya A, Tomita Y, Kuwajima G, Abraham WM, Deguchi M, Arimura A, Shichijo M. Effect of the potent and selective DP1 receptor antagonist, asapiprant (S-555739), in animal models of allergic rhinitis and allergic asthma. Eur J Pharmacol. 2015 Oct 15;765:15-23. doi: 10.1016/j.ejphar.2015.08.003. Epub 2015 Aug 12. PMID: 26277322.
In vitro protocol: TBD
In vivo protocol: 1. Takahashi G, Asanuma F, Suzuki N, Hattori M, Sakamoto S, Kugimiya A, Tomita Y, Kuwajima G, Abraham WM, Deguchi M, Arimura A, Shichijo M. Effect of the potent and selective DP1 receptor antagonist, asapiprant (S-555739), in animal models of allergic rhinitis and allergic asthma. Eur J Pharmacol. 2015 Oct 15;765:15-23. doi: 10.1016/j.ejphar.2015.08.003. Epub 2015 Aug 12. PMID: 26277322.

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1: Wong LR, Zheng J, Wilhelmsen K, Li K, Ortiz ME, Schnicker NJ, Thurman A, Pezzulo AA, Szachowicz PJ, Li P, Pan R, Klumpp K, Aswad F, Rebo J, Narumiya S, Murakami M, Zuniga S, Sola I, Enjuanes L, Meyerholz DK, Fortney K, McCray PB Jr, Perlman S. Eicosanoid signalling blockade protects middle-aged mice from severe COVID-19. Nature. 2022 May;605(7908):146-151. doi: 10.1038/s41586-022-04630-3. Epub 2022 Mar 21. PMID: 35314834; PMCID: PMC9783543.


2: Takahashi G, Asanuma F, Suzuki N, Hattori M, Sakamoto S, Kugimiya A, Tomita Y, Kuwajima G, Abraham WM, Deguchi M, Arimura A, Shichijo M. Effect of the potent and selective DP1 receptor antagonist, asapiprant (S-555739), in animal models of allergic rhinitis and allergic asthma. Eur J Pharmacol. 2015 Oct 15;765:15-23. doi: 10.1016/j.ejphar.2015.08.003. Epub 2015 Aug 12. PMID: 26277322.


3: Goldwaser E, Laurent C, Lagarde N, Fabrega S, Nay L, Villoutreix BO, Jelsch C, Nicot AB, Loriot MA, Miteva MA. Machine learning-driven identification of drugs inhibiting cytochrome P450 2C9. PLoS Comput Biol. 2022 Jan 26;18(1):e1009820. doi: 10.1371/journal.pcbi.1009820. PMID: 35081108; PMCID: PMC8820617.


4: Santini G, Mores N, Malerba M, Mondino C, Macis G, Montuschi P. Investigational prostaglandin D2 receptor antagonists for airway inflammation. Expert Opin Investig Drugs. 2016 Jun;25(6):639-52. doi: 10.1080/13543784.2016.1175434. Epub 2016 Apr 25. PMID: 27094922.


5: Roy Wong LY, Zheng J, Wilhelmsen K, Li K, Ortiz ME, Schnicker NJ, Pezzulo AA, Szachowicz PJ, Klumpp K, Aswad F, Rebo J, Narumiya S, Murakami M, Meyerholz DK, Fortney K, McCray PB, Perlman S. Eicosanoid signaling as a therapeutic target in middle-aged mice with severe COVID-19. bioRxiv [Preprint]. 2021 Apr 21:2021.04.20.440676. doi: 10.1101/2021.04.20.440676. PMID: 33907749; PMCID: PMC8077574.