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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 | Price | Availability | Quantity |
---|---|---|---|
1 mg | $55 | In Stock | |
5 mg | $133 | In Stock | |
10 mg | $239 | In Stock | |
25 mg | $350 | In Stock | |
50 mg | $523 | In Stock | |
100 mg | $759 | In Stock | |
500 mg | $1,580 | In Stock | |
1 mL x 10 mM (in DMSO) | $137 | In Stock |
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 | DP1 (human):850 nM(EC50), IP (rat):530 nM(EC50), IP (human):8.5 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]. |
Alias | APD811 |
Molecular Weight | 431.91 |
Formula | C23H26ClNO5 |
Cas No. | 1187856-49-0 |
Smiles | OC(=O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(Cl)cc2)CC1 |
Relative Density. | no data available |
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) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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