1. GPCR/G Protein
  2. Prostaglandin Receptor

Asapiprant (Synonyms: S-555739)

Cat. No.: HY-16763 Purity: 99.67%
Handling Instructions

Asapiprant is a potent and selective DP1 receptor antagonist with a Ki of 0.44 nM.

For research use only. We do not sell to patients.

Asapiprant Chemical Structure

Asapiprant Chemical Structure

CAS No. : 932372-01-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 596 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 540 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 780 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
50 mg USD 2340 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg USD 3540 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Asapiprant is a potent and selective DP1 receptor antagonist with a Ki of 0.44 nM.

IC50 & Target

Ki: 0.44 nM (DP1 receptor)[1]

In Vivo

Oral administration of Asapiprant to sheep at 1 and 3 mg/kg significantly (P<0.01) suppresses the increase in nasal resistance by 82% and 92%, respectively. Oral administration of Asapiprant to sheep at 5 mg/kg suppresses Prostaglandin (PG) D2 (PGD)2-induced nasal resistance by 86%. When orally administered 1 h before the antigen challenge in pigs, Asapiprant (3, 10, and 30 mg/kg) suppresses immediate airway response (IAR) by 52%, 57%, and 96%, and late airway response (LAR) by 67%, 50%, and 79%, respectively. Orally administered with Asapiprant (5 mg/kg) for 4 days, the Asapiprant significantly (P<0.01) suppresses antigen-induced nasal resistance by 73% in sheep. Treatment with 3 and 30 mg/kg of Asapiprant in pigs significantly (P<0.01) suppresses nasal secretion by 53% and 72%, respectively. Treatment with Asapiprant in rats at 10 mg/kg significantly (P<0.05) reduces airway hyper-responsiveness (AHR), infiltration of inflammatory cells, and mucin production in bronchoalveolar lavage fluid (BALF), although treatment with Asapiprant at 0.1 mg/kg does not have a significant effect on any responses[1].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.9938 mL 9.9691 mL 19.9382 mL
5 mM 0.3988 mL 1.9938 mL 3.9876 mL
10 mM 0.1994 mL 0.9969 mL 1.9938 mL
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[1]

Male Hartley guinea pigs (300 to 400 g) and male brown Norway rats (240 to 400 g) are used in this study. The guinea pigs and rats are housed in an air-conditioned room at 20 to 26°C with a relative humidity of 30 to 70%, and are fed standard laboratory chow and given water ad libitum. Female sheep (32 to 46 kg) naturally sensitive to ascaris suum antigen are also used. After the oral administration of Asapiprant to rats, guinea pigs, and sheep at 10 mg/kg in suspension with 0.5% methylcellulose solution, the plasma concentrations of the drugs are measured[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

501.55

Formula

C₂₄H₂₇N₃O₇S

CAS No.

932372-01-5

SMILES

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

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

10 mM in DMSO

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

Purity: 99.67%

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Asapiprant
Cat. No.:
HY-16763
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