An IP receptor antagonist
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RO3244794

Item No. 25350

Product Insert (PDF)
Technical Information
Formal Name
4-fluoro-N-[[[5-(4-fluorophenyl)-2-benzofuranyl]methoxy]carbonyl]-D-phenylalanine
CAS Number
361457-01-4
Molecular Formula
C25H19F2NO5
Formula Weight
Purity
≥98%
A solid
DMSO: Soluble: ≥ 10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
O=C([C@H](NC(OCC1=CC2=CC(C3=CC=C(C=C3)F)=CC=C2O1)=O)CC4=CC=C(C=C4)F)O
InChi Code
InChI=1S/C25H19F2NO5/c26-19-6-1-15(2-7-19)11-22(24(29)30)28-25(31)32-14-21-13-18-12-17(5-10-23(18)33-21)16-3-8-20(27)9-4-16/h1-10,12-13,22H,11,14H2,(H,28,31)(H,29,30)/t22-/m1/s1
InChi Key
IDONYPMIPXYFLY-JOCHJYFZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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.

    References & Product Citations
    Product Description References

    1. Bley, K.R., Bhattacharya, A., Daniels, D.V., et alRO1138452 and RO3244794: Characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists. Br. J. Pharmacol. 147(3), 335-345 (2006).

    2. Orie, N.N., Ledwozyw, A., Williams, D.J., et alDifferential actions of the prostacyclin analogues treprostinil and iloprost and the selexipag metabolite, MRE-269 (ACT-333679) in rat small pulmonary arteries and veins. Prostaglandins Other Lipid Mediat. 106, 1-7 (2013).

    3. Tourdot, B.E., Adili, R., Isingizwe, Z.R., et al12-HETrE inhibits platelet reactivity and thrombosis in part through the prostacyclin receptor. Blood Adv. 1(15), 1124-1131 (2017).