Aprocitentan
CAS No. : 1103522-45-7
(Synonyms: ACT-132577)
| Size | Price | Stock |
|---|---|---|
| 1mg | $58 | In-stock |
| 5mg | $144 | In-stock |
| 10mg | $209 | In-stock |
| 50mg | $511 | In-stock |
| 100mg | $690 | In-stock |
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| Cat. No. : | HY-15895 |
| M.Wt: | 546.19 |
| Formula: | C16H14Br2N6O4S |
| Purity: | >98 % |
| Solubility: | DMSO : 25 mg/mL (ultrasonic;warming;heat to 60°C) |
Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent[1]. In Vitro:Aprocitentan (ACT-132577) achieves full inhibition of intracellular calcium increase induced by ET-1 on nonrecombinant cells (primary human pulmonary smooth muscle cells and rat aortic smooth muscle cell line A10 and mouse fibroblast cell line 3T3)[1]. In Vivo:Aprocitentan (ACT-132577) has a volume of distribution greater than the plasma volume and a longer half-life than its parent compound in the rat[1]. In rat plasma, the mean recovery of Aprocitentan (ACT-132577) ranges from 82.6% to 90.6%, matrix effect of Aprocitentan (ACT-132577) in rat plasma ranges from 101.4% to 115.2%[2].
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