ACT-132577
- Product Name
- ACT-132577
- CAS No.
- 1103522-45-7
- Chemical Name
- ACT-132577
- Synonyms
- ACT-132577;Aprocitentan;Depropylmethacetin;Despropyl Macitentan;Macitentan ACT-132577;N-Despropyl Macitentan;Macitentan Impurity 07;Macitentan ACT-132577-D4;D4-N-Despropyl Macitentan;Aprocitentan, 10 mM in DMSO
- CBNumber
- CB12685914
- Molecular Formula
- C16H14Br2N6O4S
- Formula Weight
- 546.19
- MOL File
- 1103522-45-7.mol
ACT-132577 Property
- Melting point:
- 139-141°C
- Boiling point:
- 705.0±70.0 °C(Predicted)
- Density
- 1.841±0.06 g/cm3(Predicted)
- storage temp.
- -20°C Freezer
- solubility
- Chloroform (Slightly, Heated), Methanol (Slightly, Heated)
- form
- Solid
- pka
- 13.56±0.60(Predicted)
- color
- White to Off-White
- InChI
- InChI=1S/C16H14Br2N6O4S/c17-11-3-1-10(2-4-11)13-14(24-29(19,25)26)22-9-23-15(13)27-5-6-28-16-20-7-12(18)8-21-16/h1-4,7-9H,5-6H2,(H2,19,25,26)(H,22,23,24)
- InChIKey
- DKULOVKANLVDEA-UHFFFAOYSA-N
- SMILES
- S(NC1C(C2=CC=C(Br)C=C2)=C(OCCOC2=NC=C(Br)C=N2)N=CN=1)(N)(=O)=O
N-Bromosuccinimide Price
- Product number
- D297305
- Product name
- N-DespropylMacitentan
- Packaging
- 10mg
- Price
- $580
- Updated
- 2021/12/16
- Product number
- D297305
- Product name
- N-DespropylMacitentan
- Packaging
- 5mg
- Price
- $305
- Updated
- 2021/12/16
- Product number
- D297305
- Product name
- N-DespropylMacitentan
- Packaging
- 50mg
- Price
- $1635
- Updated
- 2021/12/16
- Product number
- CS-2687
- Product name
- Aprocitentan
- Purity
- 98.13%
- Packaging
- 100mg
- Price
- $2520
- Updated
- 2021/12/16
- Product number
- CS-2687
- Product name
- Aprocitentan
- Purity
- 98.13%
- Packaging
- 5mg
- Price
- $420
- Updated
- 2021/12/16
ACT-132577 Chemical Properties,Usage,Production
Uses
N-Despropyl-macitentan, is an active metabolite which is part of a family of endothelin receptor antagonist that allows for treatment of pulmonary arterial hypertension (PAH)
Definition
ChEBI: ACT-132577 is a member of the class of sulfamides in which one of the amino groups of sulfonamide is substituted by a 5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl group. An active metabolite of macitentan (obtained by oxidative depropylation), an orphan drug used for the treatment of pulmonary arterial hypertension. It has a role as an antihypertensive agent, an endothelin receptor antagonist, a drug metabolite and a xenobiotic metabolite. It is an aromatic ether, an organobromine compound, a member of pyrimidines and a member of sulfamides. It is functionally related to an ethylene glycol.
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].
IC 50
ETA: 3.4 nM (IC50); ETA: 6.7 (pA2); ETB: 987 nM (IC50); ETB: 5.5 (pA2)
ACT-132577 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from ACT-132577 manufacturers
- Product
- Aprocitentan 1103522-45-7
- Price
- US $0.00/kg
- Min. Order
- 25kg
- Purity
- 0.99
- Supply Ability
- /
- Release date
- 2025-11-04
- Product
- Aprocitentan 1103522-45-7
- Price
- US $0.00-0.00/g
- Min. Order
- 1g
- Purity
- 99%
- Supply Ability
- 1000
- Release date
- 2024-05-28