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1187856-49-0

1187856-49-0 structure
1187856-49-0 structure
  • Name: Ralinepag
  • Chemical Name: Ralinepag
  • CAS Number: 1187856-49-0
  • Molecular Formula: C23H26ClNO5
  • Molecular Weight: 431.909
  • Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
  • Create Date: 2018-10-17 19:30:57
  • Modify Date: 2024-01-19 06:50:03
  • Ralinepag is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively.

Name Ralinepag
Synonyms {[trans-4-({[(4-Chlorophenyl)(phenyl)carbamoyl]oxy}methyl)cyclohexyl]methoxy}acetic acid
10029
APD811
CQY12ZJN6E
2-[[trans-4-[[[(4-chlorophenyl)(phenyl)carbamoyl]oxy]methyl]cyclohexyl]methoxy]acetic acid
MFCD28502072
Ralinepag
Acetic acid, 2-[[trans-4-[[[[(4-chlorophenyl)phenylamino]carbonyl]oxy]methyl]cyclohexyl]methoxy]-
UNII-CQY12ZJN6E
Description Ralinepag is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively.
Related Catalog
Target

hIP:8.5 nM (EC50)

rIP:530 nM (EC50)

In Vitro Ralinepag is a potent non-prostanoid prostacyclin receptor agonist, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively. 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, p.o.) markedly reduces the monocrotaline (MCT)-induced increase in pulmonary arterial pressure and pulmonary vessel wall thickness in rats[1].
References

[1]. Tran TA, et al. Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. J Med Chem. 2017 Feb 9;60(3):913-927.

Density 1.3±0.1 g/cm3
Boiling Point 609.1±35.0 °C at 760 mmHg
Molecular Formula C23H26ClNO5
Molecular Weight 431.909
Flash Point 322.2±25.9 °C
Exact Mass 431.149963
LogP 4.86
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.582
Storage condition -20℃