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CAS No. : 1187856-49-0
MCE 国际站:Ralinepag
产品活性:Ralinepag 是一种有效的,可口服的,非前列腺素类 prostacyclin (IP) receptor 激动剂,对人和大鼠的 IP 受体的 EC50 值分别为 8.5 nM 和 530 nM,对人 DP1 受体的 EC50 值为 850 nM。
研究领域:GPCR/G Protein
作用靶点:Prostaglandin Receptor
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.
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.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Anti-Cardiovascular Disease Compound Library | Endocrinology Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | Angiogenesis-Related Compound Library | Targeted Diversity Library | Rare Diseases Drug Library | Coagulation and Anti-coagulation Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Activators Library | CAY10580 | EP3 antagonist 3 | Dinoprost-d4 | TCS 2510 | Vidupiprant | EP2 receptor antagonist-1 | FR181157 | SC 51089 | SC-51322 | Misoprostol acid | Treprostinil sodium | Aganepag isopropyl | Prostaglandin E2 | Taprostene | Cicaprost | Fevipiprant | Carboprost | TG6-10-1 | Latanoprost acid | Carbacyclin | KW-8232 free base | Nocloprost | Cloprostenol isopropyl ester | ICI 192605 | HHS-0701 | Bimatoprost-d5 | AS604872
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