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Ralinepag

Cat. No. M10253
Ralinepag Structure
Synonym:

APD811

Size Price Availability Quantity
5mg USD 148.5  USD165 In stock
10mg USD 261  USD290 In stock
25mg USD 603  USD670 In stock
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Quality Control
  • Current batch:
  • Purity >99.5%
  • COA
  • MSDS
Biological Activity

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. Ralinepag also inhibits the ADP-induced human platelet aggregation, with an IC50 of 38 nM. 

In vivo, Ralinepag (30 mg/kg; p.o.) markedly reduces the monocrotaline (MCT)-induced increase in pulmonary arterial pressure and pulmonary vessel wall thickness in rats.

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 431.91
Formula C23H26ClNO5
CAS Number 1187856-49-0
Purity >99.5%
Solubility DMSO ≥ 90 mg/mL
Storage at -20°C
References

Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension
Thuy-Anh Tran, et al. J Med Chem. 2017 Feb 9;60(3):913-927. PMID: 28072531.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Ralinepag, APD811 supplier, Prostaglandin Receptor, inhibitors

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