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Asapiprant

Cat. No. M9464
Asapiprant Structure
Synonym:

S-555739; CS-2811

Size Price Availability Quantity
2mg USD 310  USD310 In stock
5mg USD 495  USD495 In stock
10mg USD 710  USD710 In stock
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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

[1] Takahashi G, et al. Eur J Pharmacol. Effect of the potent and selective DP1 receptor antagonist, asapiprant (S-555739), in animal models of allergic rhinitis and allergic asthma.

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  Catalog
Abmole Inhibitor Catalog 2017




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

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