Free shipping on all orders over $ 500

Asapiprant

Cat. No. M9464
Asapiprant Structure
Synonym:

S-555739; CS-2811

Size Price Availability Quantity
2mg USD 279  USD310 In stock
5mg USD 445.5  USD495 In stock
10mg USD 639  USD710 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Asapiprant is a potent and selective DP1 receptor antagonist, with a Ki of 0.44 nM. Asapiprant exhibited high affinity and selectivity for the DP1 receptor. 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. 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 501.55
Formula C24H27N3O7S
CAS Number 932372-01-5
Purity >99%
Solubility DMSO ≥ 6 mg/mL
Storage at -20°C
References

Effect of the potent and selective DP1 receptor antagonist, asapiprant (S-555739), in animal models of allergic rhinitis and allergic asthma.
Takahashi G, et al. Eur J Pharmacol. 2015 Oct 15;765:15-23. PMID: 26277322.

Related Prostaglandin Receptor Products
Omidenepag

Omidenepag,a pharmacologically active form of Omidenepag Isopropyl, is a selective, non-prostanoid EP2 receptor agonist, with an EC50 of 1.1 nM.

Ralinepag

Ralinepag (APD811) is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist with EC50 of 8.5 nM, 530 nM and 850 nM for human IP receptor, rat IP receptor and human DP1 receptor, respectively.

GW627368X

GW627368X is a novel, potent and selective competitive antagonist of prostanoid EP4 receptors with additional human TP receptor affinity.

Taprenepag

Taprenepag, also known as CP-544326, is a potent and selective EP(2) receptor agonist, with IC50 values of 10 and 15 nM for human and rat EP2, respectively.

Darbufelone

Darbufelone is a dual inhibitor of cellular PGF2α and LTB4 production, it is also a COX-2 inhibitor potentially for the treatment of rheumatoid arthritis.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Asapiprant, S-555739; CS-2811 supplier, Prostaglandin Receptor, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.