Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 55.00 | |
5 mg | In stock | $ 133.00 | |
10 mg | In stock | $ 239.00 | |
25 mg | In stock | $ 350.00 | |
50 mg | In stock | $ 523.00 | |
100 mg | In stock | $ 759.00 | |
500 mg | In stock | $ 1,580.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 137.00 |
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. |
Targets&IC50 | IP (human):8.5 nM(EC50), IP (rat):530 nM(EC50), DP1 (human):850 nM(EC50) |
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]. |
Synonyms | APD811 |
Molecular Weight | 431.91 |
Formula | C23H26ClNO5 |
CAS No. | 1187856-49-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL
You can also refer to dose conversion for different animals. More
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Ralinepag 1187856-49-0 GPCR/G Protein Immunology/Inflammation Others Prostaglandin Receptor inhibit APD 811 Inhibitor APD-811 APD811 inhibitor