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Ralinepag

Catalog No. T4635 CAS 1187856-49-0

Synonyms: 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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Ralinepag, CAS 1187856-49-0

Pack Size	Availability	Price/USD
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

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Purity: 99.85%

Purity: 99.41%

Biological Description

Chemical Properties

Storage & Solubility Information

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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Immunology/Inflammation Compound Library NO PAINS Compound Library Anti-Cardiovascular Disease Compound Library Anti-Hypertension Compound Library Orally Active Compound Library Anti-Aging Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Ralinepag 1187856-49-0 GPCR/G Protein Immunology/Inflammation Others Prostaglandin Receptor inhibit APD 811 Inhibitor APD-811 APD811 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.