| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
With EC50 values of 8.5 nM, 530 nM, and 850 nM for human and rat IP receptors and human DP1 receptors, respectively, ralinepag is a strong non-prostacyclin receptor agonist. With Kis of 1.2 nM, 3 nM, 76 nM, and 256 nM for monkey, human, rat, and dog IP receptors (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, Ralinepag (5c) exhibits a strong affinity for prostaglandin receptors. Ralinepag also did not affect the functional activity of the hERG channel (IC50 > 30 μM) or the cytochrome P450 enzymes (IC50 > 50 μM for CYP 1A2, 2D6, 3A4, 2C8, 2C9, and 2C19) in patch clamp experiments. With an IC50 of 38 nM, ralinepag also prevents human platelet aggregation triggered by ADP [1].
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| ln Vivo |
In rats, monocrotaline (MCT)-induced elevations in pulmonary artery pressure and pulmonary vascular wall thickness can be considerably attenuated by ralingepag (30 mg/kg, orally) [1].
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| References | |
| Additional Infomation |
Ralinepag has been used in trials studying the treatment of Pulmonary Arterial Hypertension.
Drug Indication Treatment of pulmonary arterial hypertension |
| Molecular Formula |
C23H26CLNO5
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|---|---|
| Molecular Weight |
431.909245967865
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| Exact Mass |
431.15
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| CAS # |
1187856-49-0
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| Related CAS # |
1187856-49-0;1187857-75-5 (sodium);
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| PubChem CID |
44219292
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| Appearance |
White to off-white solid powder
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| LogP |
5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
30
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| Complexity |
538
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(O)(=O)COC[C@@H]1CC[C@@H](COC(N(C2=CC=C(Cl)C=C2)C2=CC=CC=C2)=O)CC1
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| InChi Key |
NPDKXVKJRHPDQT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H26ClNO5/c24-19-10-12-21(13-11-19)25(20-4-2-1-3-5-20)23(28)30-15-18-8-6-17(7-9-18)14-29-16-22(26)27/h1-5,10-13,17-18H,6-9,14-16H2,(H,26,27)
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| Chemical Name |
2-[[4-[[(4-chlorophenyl)-phenylcarbamoyl]oxymethyl]cyclohexyl]methoxy]acetic acid
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| Synonyms |
APD811; APD 811; APD-811
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~231.53 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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