1103522-45-7
- Product Name：Aprocitentan
- Molecular Formula：C16H14Br2N6O4S
- Purity：99%
- Molecular Weight：546.199
Product Details:
CasNo： 1103522-45-7
Molecular Formula： C16H14Br2N6O4S
Hot Sale Factory Supply High Purity Aprocitentan 1103522-45-7 Lowest Price
- Molecular Formula:C16H14Br2N6O4S
- Molecular Weight:546.199
- Boiling Point:705.0±70.0 °C(Predicted)
- PKA:13.56±0.60(Predicted)
- PSA：150.59000
- Density:1.841±0.06 g/cm3(Predicted)
- LogP:4.38590
Aprocitentan(Cas 1103522-45-7) Usage
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Description |
Aprocitentan (ACT-132577) is an investigational oral medication, administered once daily, that functions as a dual endothelin receptor antagonist (ERA). It is taken orally and is a metabolite derived from macitentan. As a dual ERA, aprocitentan acts on both endothelin A (ETA) and endothelin B (ETB) receptors. Its mechanism of action is deemed suitable for addressing challenging forms of hypertension, and it has the potential to enhance the effects of other antihypertensive drugs, suggesting possible long-term benefits. |
| Uses | A Phase 3 study has demonstrated the safety and efficacy of aprocitentan in reducing blood pressure, particularly in patients with resistant hypertension. Notably, aprocitentan was found to significantly lower blood pressure when used in conjunction with at least three antihypertensive medications, including a diuretic. Aprocitentan is also recognized as an active metabolite of macitentan, obtained through oxidative depropylation. Macitentan itself is an orphan drug employed in the treatment of pulmonary arterial hypertension. Aprocitentan exhibits high binding to plasma proteins and undergoes elimination through both urine and feces. |
1103522-45-7 Relevant articles
CRYSTALLINE FORMS OF A 4-PYRIMIDINESULFAMIDE DERIVATIVE APROCITENTAN
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Paragraph 0231, (2020/01/22)
The present invention concerns novel cry...
COMBINATION OF A 4-PYRIMIDINESULFAMIDE DERIVATIVE WITH AN SGLT-2 INHIBITOR FOR THE TREATMENT OF ENDOTHELIN RELATED DISEASES
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Page/Page column 38, (2019/06/17)
The present invention concerns the compo...
PROCESS FOR MANUFACTURING PYRIMIDINE SULFAMIDE DERIVATIVES
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Page/Page column 45, (2015/09/22)
The invention relates to a process for m...
Aprocitentan, A Dual Endothelin Receptor Antagonist Under Development for the Treatment of Resistant Hypertension
Fabio Angeli, Paolo Verdecchia & Gianpaolo Reboldi
, Cardiology and Therapy, Volume 10, pages 397–406, (2021)
Significant changes in BP with aprocitentan are observed within 14 days, and its BP-lowering effects have also been documented with ambulatory BP monitoring.
1103522-45-7 Process route
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5-(4-bromophenyl)-4-(2-((5-bromopyrimidin-2-yl)oxy)ethoxy)-6-fluoropyrimidine
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- 1103522-45-7
ACT-132577
| Conditions | Yield |
|---|---|
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With potassium carbonate; SULFAMIDE; In dimethyl sulfoxide; at 70 ℃; for 3h; Solvent;
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84% |
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With potassium carbonate; SULFAMIDE; In water; dimethyl sulfoxide; at 70 - 75 ℃; for 4h; Time; Temperature;
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77% |
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With potassium carbonate; SULFAMIDE; In dimethyl sulfoxide; at 70 ℃; for 3h; Reagent/catalyst;
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65% |
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5-(4-bromophenyl)-4-(2-((5-bromopyrimidin-2-yl)oxy)ethoxy)-6-chloropyrimidine
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- 1103522-45-7
ACT-132577
| Conditions | Yield |
|---|---|
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5-(4-bromophenyl)-4-(2-((5-bromopyrimidin-2-yl)oxy)ethoxy)-6-chloropyrimidine; With cesium fluoride; In dimethyl sulfoxide; at 70 ℃; for 2.5h;
With potassium carbonate; SULFAMIDE; In dimethyl sulfoxide; for 3h; Reagent/catalyst; Heating;
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77% |
1103522-45-7 Upstream products
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441796-09-4
benzylsulfamic acid {5-(4-bromophenyl)-6-[2-(5-bromopyrimidin-2-yloxy)-ethoxy]-pyrimidine-4-yl}-amide
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(4-bromo-phenyl)-acetic acid methyl ester
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1878-68-8
2-(4-bromophenyl)-acetic acid
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146533-41-7
5-(4-bromophenyl)-4,6-dichloropyrimidine
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