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Aprocitentan

Chemical Structure : Aprocitentan

CAS No.: 1103522-45-7

Aprocitentan (ACT-132577, ACT132577)

Catalog No.: PC-60030Not For Human Use, Lab Use Only.

Aprocitentan (ACT132577) is the major and pharmacologically active metabolite of Macitentan, an orally active, dual endothelin receptor antagonist with IC50s of 3.4 nM and 987 nM for ETA/ETB receptor respectively, inhibits ET-1 and ET-2-induced contractions in functional assays.

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Biological Activity

Aprocitentan (ACT132577) is the major and pharmacologically active metabolite of Macitentan, an orally active, dual endothelin receptor antagonist with IC50s of 3.4 nM and 987 nM for ETA/ETB receptor respectively, inhibits ET-1 and ET-2-induced contractions in functional assays.

Physicochemical Properties

M.Wt 546.194
Formula C16H14Br2N6O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl]sulfuric diamide

References

1. Iglarz M, et al. J Pharmacol Exp Ther. 2008 Dec;327(3):736-45.

2. Kummer O, et al. Eur J Pharm Sci. 2009 Nov 5;38(4):384-8.

3. Sidharta PN, et al. Eur J Clin Pharmacol. 2011 Oct;67(10):977-84.

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