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Ralinepag

SKU: orb1302695

Description

Ralinepag (APD811) is a potent, orally active non-prostanoid IP receptor agonist, exhibiting EC50 values of 8.5 nM (human IP), 530 nM (rat IP), and 850 nM (human DP1). It is a research tool used in vitro and in vivo to study pulmonary arterial hypertension and other IP receptor-mediated pathways.

Research Area

Immunology & Inflammation, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number1187856-49-0
MW431.91
Purity99.85%
FormulaC23H26ClNO5
SMILESOC(=O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(Cl)cc2)CC1
TargetProstaglandin Receptor
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.63 mM);DMSO:55 mg/mL (127.34 mM)

Bioactivity

Target IC50
IP (human):8.5 nM(EC50)|DP1 (human):850 nM(EC50)|IP (rat):530 nM(EC50)
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).
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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

APD811, APD-811, APD 811, Inhibitor, inhibit, Prostaglandin Receptor, ProstaglandinReceptor, Prostacyclin receptor, Ralinepag

Similar Products

  • Ralinepag [orb1222829]

    >98% (HPLC)

    1187856-49-0

    431.9

    C23H26ClNO5

    50 mg, 100 mg, 500 mg, 5 mg, 1 g, 10 mg, 25 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Key Properties

No computed properties available.

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Ralinepag (orb1302695)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
¥ 1,170.00
2 mg
¥ 1,430.00
5 mg
¥ 2,080.00
1 ml x 10 mM (in DMSO)
¥ 2,340.00
10 mg
¥ 2,990.00
25 mg
¥ 4,680.00
50 mg
¥ 6,630.00
100 mg
¥ 9,230.00
200 mg
¥ 12,740.00
DispatchUsually dispatched within 3-5 working days
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