1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. Ralinepag

Ralinepag (Synonyms: APD811)

Cat. No.: HY-16751 Purity: 98.87%
Handling Instructions

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.

For research use only. We do not sell to patients.

Ralinepag Chemical Structure

Ralinepag Chemical Structure

CAS No. : 1187856-49-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1850 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2850 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

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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.

IC50 & Target[1]

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].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (289.41 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3153 mL 11.5765 mL 23.1530 mL
5 mM 0.4631 mL 2.3153 mL 4.6306 mL
10 mM 0.2315 mL 1.1576 mL 2.3153 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

431.91

Formula

C₂₃H₂₆ClNO₅

CAS No.

1187856-49-0

SMILES

O=C(O)COC[[email protected]]1CC[[email protected]](COC(N(C2=CC=C(Cl)C=C2)C3=CC=CC=C3)=O)CC1

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Ralinepag
Cat. No.:
HY-16751
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Ralinepag

Cat. No.: HY-16751