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Ralinepag

🥰Excellent
Catalog No. T4635Cas No. 1187856-49-0
Alias APD811

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.

Ralinepag

Ralinepag

🥰Excellent
Purity: 99.85%
Catalog No. T4635Alias APD811Cas No. 1187856-49-0
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 SizePriceAvailabilityQuantity
1 mg$55In Stock
5 mg$133In Stock
10 mg$239In Stock
25 mg$350In Stock
50 mg$523In Stock
100 mg$759In Stock
500 mg$1,580In Stock
1 mL x 10 mM (in DMSO)$137In Stock
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Purity:99.85%
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Product Introduction

Bioactivity
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].
AliasAPD811
Chemical Properties
Molecular Weight431.91
FormulaC23H26ClNO5
Cas No.1187856-49-0
SmilesOC(=O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(Cl)cc2)CC1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.3153 mL11.5765 mL23.1530 mL115.7649 mL
5 mM0.4631 mL2.3153 mL4.6306 mL23.1530 mL
10 mM0.2315 mL1.1576 mL2.3153 mL11.5765 mL
20 mM0.1158 mL0.5788 mL1.1576 mL5.7882 mL
50 mM0.0463 mL0.2315 mL0.4631 mL2.3153 mL
100 mM0.0232 mL0.1158 mL0.2315 mL1.1576 mL

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