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Ralinepag

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Chemical Structure| 1187856-49-0 同义名 : APD811
CAS号 : 1187856-49-0
货号 : A336258
分子式 : C23H26ClNO5
纯度 : 99%+
分子量 : 431.909
MDL号 : MFCD28502072
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(243.11 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Ralinepag is a potent non-prostanoid prostacyclin receptor agonist, demonstrating exceptional efficacy with EC50 values of 8.5 nM for both human and rat IP receptors, and a slightly higher affinity for the human DP1 receptor with an EC50 of 850 nM. Its receptor binding affinity is significant across various species for the prostaglandin receptor, displaying Kis of 1.2 nM in monkeys, 3 nM in humans, 76 nM in rats, and 256 nM in dogs for the IP receptor using the ligand [3H]-iloprost. Additionally, Ralinepag exhibits binding affinities with Kis of 2.6 μM for human DP1, 9.6 μM for EP1, 610 nM for EP2, 143 nM for EP3v6, and 678 nM for EP4 receptors, employing [3H]-PGE2 as the ligand. Importantly, Ralinepag does not significantly affect cytochrome P450 enzymes, with IC50 values exceeding 50 μM for enzymes including CYPs 1A2, 2D6, 3A4, 2C8, 2C9, and 2C19, nor does it impact hERG channel functional activity in patch clamp assays, with an IC50 surpassing 30 μM. Moreover, Ralinepag efficiently inhibits ADP-induced human platelet aggregation, demonstrating an IC50 of 38 nM[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.58mL

2.32mL

1.16mL

23.15mL

4.63mL

2.32mL
参考文献

[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.