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Aprocitentan

Aprocitentan is a dual endothelin type A (ETA) and ETB receptor antagonist and an active metabolite of macitentan.<sup class="referenceList">[1]</sup> It is formed from macitentan by the cytochrome P450 (CYP) isoform CYP3A4. Aprocitentan inhibits increases in intracellular calcium induced by endothelin-1 (ET-1) in primary human pulmonary arterial smooth muscle cells (HPASMCs; IC50 = 14 nM), ET-1-induced contractions in isolated rat aortic rings (pA2 = 6.7 for ETA), and sarafotoxin S6c-induced contractions of isolated rat tracheal rings (pKB = 5.5 for ETB).<sup class="referenceList">[2]</sup> It reduces ET-1-induced increases in the proliferation of isolated human skin fibroblasts when used at concentrations of 10 and 100 µM.<sup class="referenceList">[3]</sup> Aprocitentan (10-300 mg/kg) increases plasma ET-1 concentrations in normotensive rats and decreases mean arterial pressure (MAP) in DOCA-salt hypertensive rats.<sup class="referenceList">[4]</sup>
1103522-45-7
Item No.
TX008UIX
CAS No.
1103522-45-7
Molecular Formula
C16H14Br2N6O4S
Molecular Weight
546.19316
Pricing ＆ Availability
Pack Size Purity Price(USD) Availability Quantity
1mg 95% $40.00 in stock
5mg 95% $89.00 in stock
10mg 95% $134.00 in stock
25mg 95% $246.00 in stock
50mg 95% $296.00 in stock
100mg 95% $465.00 in stock
200mg 95% $700.00 in stock
WARNING This product is for research use only. SDS
Technical Information
Item No.:
TX008UIX
Product Name:
Aprocitentan
Description:
Synonyms:
ACT-132577; Aprocitentan
CAS Number:
1103522-45-7
MDL:
MFCD28155267
Molecular Formula:
C16H14Br2N6O4S
Molecular Weight:
546.19316
SMILES:
O=S(N)(NC1=NC=NC(OCCOC2=NC=C(C=N2)Br)=C1C3=CC=C(C=C3)Br)=O
λmax:
259 nm
IC₅₀ & Target:
ETA ETB
6.7 (pA2) 5.5 (pA2)
Solubility:
DMSO: soluble
Shipping Condition:
Room temperature in continental US; may vary elsewhere.
References & Citations:
[1]. 1.Iglarz, M., Binkert, C., Morrison, K., et al. Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist J. Pharmacol. Exp. Ther. 327(3),736-745 (2008).
[2]. Cutolo, M., Montagna, P., Brizzolara, R., et al. Effects of macitentan and its active metabolite on cultured human systemic sclerosis and control skin fibroblasts J. Rheumatol. 42(3),456-463 (2015).
[3]. Trensz, F., Bortolamiol, C., Kramberg, M., et al. Pharmacological characterization of aprocitentan, a dual endothelin receptor antagonist, alone and in combination with blockers of the renin angiotensin system, in two models of experimental hypertension J. Pharmacol. Exp. Ther. 368(3),462-473 (2019).
[4]. Dingemanse, J., Sidharta, P.N., Maddrey, W.C., et al. Efficacy, safety and clinical pharmacology of macitentan in comparison to other endothelin receptor antagonists in the treatment of pulmonary arterial hypertension Expert Opin. Drug Saf. 13(3),391-405 (2013).