Chemical Structure : Pipersentan
CAS No.:
2305865-93-2
Pipersentan
(Diosuxentan)
Catalog No.: PC-25043Not For Human Use, Lab Use Only.
Pipersentan (Diosuxentan) is a potent, selective endothelin receptor A (ETA receptor) antagonist, inhibits binding of 125I-ET-1 toward recombinant ETA receptor with IC50 of 4.44 nM, >1000-fold selective over ETB receptor.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Pipersentan (Diosuxentan) is a potent, selective endothelin receptor A (ETA receptor) antagonist, inhibits binding of 125I-ET-1 toward recombinant ETA receptor with IC50 of 4.44 nM, >1000-fold selective over ETB receptor.
Pipersentan completely inhibits the high intracellular calcium induced by ET-1 in recombinant CHO and SK-N-MC cells with IC50 of 1.6 nM, >30,000-fold selective over ET B.
Pipersentan efficaciously antagonized the effects of ET-1 on pulmonary artery smooth muscle cell proliferation, migration and calcium mobilization and effectively improved right ventricular hypertrophy and pulmonary arterial pressure in both monocrotaline- and hypoxia-induced pulmonary hypertension (PH) rat models.
Physicochemical Properties
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M.Wt
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569.39
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Formula
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C20H21BrN6O7S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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Sulfamide, N-[5-(1,3-benzodioxol-5-yl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N′-(2-methoxyethyl)-
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References
1. Zeyu Zhang, et al. Front Pharmacol. 2022 Jun 20:13:920222.
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