Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.
Visit our FAQ
Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888
Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.
RO3244794 is an IP receptor antagonist (Ki = 20 nM in isolated human platelets).1 It is selective for the IP receptor over a panel of 50 receptors at 10 µM but does bind to the prostaglandin E2 (PGE2) receptor subtypes EP3 and EP4, TP receptor, and adenosine A3 receptor (Kis = 4,169, 1,820, 8,128, and 4,786 nM, respectively). RO3244794 inhibits cAMP accumulation induced by carbaprostacyclin (Item No. 18210) in CHO-K1 cells expressing the human IP receptor (IC50 = 316 nM). It prevents treprostinil-induced relaxation in U-46619-precontracted isolated rat pulmonary arteries when used at a concentration of 1 µM.2 RO3244794 (250 nM) inhibits PGI2- or 12-HETrE-induced aggregation of isolated human platelet-rich plasma.3 It decreases acetic-acid induced writhing and carrageenan-induced mechanical hyperalgesia and edema in rats.1 RO3244794 (10 mg/kg) also decreases the difference in weight distribution between the osteoarthritic and control hind paws in a rat model of sodium monoiodoacetate-induced osteoarthritis.
WARNING This product is not for human or veterinary use.
1. RO1138452 and RO3244794: Characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists. Br. J. Pharmacol. 147(3), 335-345 (2006).
2. Differential actions of the prostacyclin analogues treprostinil and iloprost and the selexipag metabolite, MRE-
3. 12-