| Name | Ralinepag |
| Description | Ralinepag (APD811) is a potent, orally bioavailable agonist of non-prostanoid prostacyclin (IP) receptor, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively. |
| In vitro | Ralinepag (5c) has potent receptor binding affinity at prostaglandin receptor, with Kis of 1.2 nM, 3 nM, 76 nM, and 256 nM for monkey, human, rat, and dog IP receptor (ligand, [3H]-iloprost), and 2.6 μM, 9.6 μM, 610 nM, 143 nM, and 678 nM for human DP1, EP1, EP2, EP3v6 and EP4 receptors (ligand, [3H]-PGE2), respectively. Moreover, Ralinepag shows no effect on cytochrome P450 enzymes (IC50 > 50 μM for CYPs 1A2, 2D6, 3A4 2C8, 2C9, and 2C19) or hERG channel functional activity in a patch clamp assay (IC50 > 30 μM). Ralinepag also inhibits the ADP-induced human platelet aggregation, with an IC50 of 38 nM[1]. |
| In vivo | Ralinepag (30 mg/kg, orally) significantly mitigates the increase in pulmonary arterial pressure and the thickening of pulmonary vessel walls in rats induced by monocrotaline (MCT)[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (127.34 mM)
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| Keywords | inhibit | APD 811 | Inhibitor | Prostaglandin Receptor | APD-811 | Ralinepag |
| Inhibitors Related | Angoroside C | Pranoprofen | Tranilast | Benorilate | Rutin | Ozagrel | Ethamsylate | Rebamipide | Evodiamine | Tebufelone | Timapiprant | p-Hydroxycinnamic acid |
| Related Compound Libraries | Nonsteroidal Anti-Inflammatory Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
