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441798-33-0 (Macitentan)

1

Identification

Macitentan Macitentan
Name Macitentan
Formula C19H20Br2N6O4S
MW 588.27
CAS No. 441798-33-0
EINECS
Smiles BrC1=CN=C(OCCOC2=C(C3=CC=C(Br)C=C3)C(NS(NCCC)(=O)=O)=NC=N2)N=C1
Synonyms ACT 064992;ACT-064992;ACT064992;
InChI InChI=1S/C19H20Br2N6O4S/c1-2-7-26-32(28,29)27-17-16(13-3-5-14(20)6-4-13)18(25-12-24-17)30-8-9-31-19-22-10-15(21)11-23-19/h3-6,10-12,26H,2,7-9H2,1H3,(H,24,25,27)
2

Introduction

Macitentan(ACT064992) is an orally active, non-peptide dual endothelin ETAand ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). IC50 value: Target: ETA/ETB receptor

Background Information

Macitentan is an orally active, non-peptide dual endothelin (ET)(A) and ET(B) receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). ......by Affix Scientific
Macitentan is an orally available dual endothelin receptor (ETR) antagonist with potential antihypertensive and antineoplastic activity. ......by BOC Sciences
Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). ......by MedChemexpress Co., Ltd.
Macitentan is an orally active, non-peptide, dual ETA/ETB (endothelin) receptor antagonist with IC50 of 0.5 nM/391 nM. ......by Selleck Chemicals LLC
Macitentan is an orally active, non-peptide, dual ETA/ETB (endothelin) receptor antagonist with IC50 of 0.5 nM/391 nM. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:White to off-white solid EBNumber:EB000023905

Storage condition

Up to one week at 4°C or six months at -20°C. by Affix Scientific

Solubility

DMSO by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 100 mg/mL (169.98 mM); Water<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM) by Selleck Chemicals LLC
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Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Macitentan Actelion Ltd Pulmonary artery hypertension 2013/9/30 2016/3/31 Phase 3 Clinical
Macitentan Actelion Ltd Pulmonary artery hypertension 2013/4/30 2014/12/31 Phase 3 Clinical
Macitentan Actelion Ltd Eisenmenger syndrome 2013/5/31 2014/6/30 Phase 3 Clinical
Macitentan Actelion Ltd Eisenmenger syndrome 2013/9/30 2016/6/30 Phase 3 Clinical
Macitentan Actelion Ltd Skin ulcer 2011/12/31 2014/5/31 Phase 3 Clinical
Macitentan - Pre-registration
Macitentan - Launched
7

Safety Data of Macitentan

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
Affix Scientific 10mg/USD758(In stock);50mg/USD1470(In stock) USA
BOC Sciences 1g/USD399(In stock)
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD180();10mg/USD336() USA
MedChemexpress Co., Ltd. 5mg/USD180();10mg/USD336() USA
Selleck Chemicals LLC 5mg/USD170(In stock);10mM/1mLIn DMSO/USD400(In stock);25mg/USD570(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD180();10mg/USD336() China
Target Molecule Corp. 10mg/USD168();25mg/USD288();50mg/USD548() USA
Utopharm Co., Ltd. China
10

Related Products

Other Forms of 441798-33-0

Name CAS No Formula MW
Macitentan (n-butyl analogue) 556797-16-1 C20H21Br2N5O4S 587.28
Macitentan (D4) 1258428-05-5 C19H16D4Br2N6O4S 592.3

Recommended Compounds in Endothelin Receptor

Name CAS No Formula MW
ACT-132577 1103522-45-7 C16H14Br2N6O4S 546.19
BQ-788 (sodium salt) 156161-89-6 C34H50N5NaO7 663.78
Sulfisoxazole 127-69-5 C11H13N3O3S 267.3
Atrasentan (hydrochloride) 195733-43-8 C29H39ClN2O6 547.08
Bosentan (hydrate) 157212-55-0 C27H31N5O7S 569.63
SPI-1620 142569-99-1 C83H112N19O25 1775.89
Atrasentan 173937-91-2 C29H38N2O6 510.62
Sitaxsentan (phosphate) 215501-46-5 C18H17ClN2O10PS2- 551.8923
Avosentan 290815-26-8 C23H21N5O5S 479.51
Zibotentan 186497-07-4 C19H16N6O4S 424.43
Ambrisentan 177036-94-1 C22H22N2O4 378.42
sitaxsentan 184036-34-8 C18H15ClN2O6S2 454.9
Bosentan 147536-97-8 C27H29N5O6S 551.61
Sitaxsentan (sodium) 210421-74-2 C18H14ClN2NaO6S2 476.89
Endothelin 1 117399-94-7 C109H159N25O32S5 2491.9
BQ-123 136553-81-6 C31H42N6O7 610.7012
Aminaftone 14748-94-8 C18H15NO4 309.32
Ro 46-2005 150725-87-4 C23H27N3O6S 473.54
ZD-1611 186497-38-1 C22H24N4O5S 456.51
Macitentan (n-butyl analogue) 556797-16-1 C20H21Br2N5O4S 587.28

Recommended Compounds in Same Indication

Name CAS No Formula MW
Sildenafil (citrate) 171599-83-0 C28H38N6O11S 666.7
sitaxsentan 184036-34-8 C18H15ClN2O6S2 454.9
Riociguat 625115-55-1 C20H19FN8O2 422.42
Sildenafil 139755-83-2 C22H30N6O4S 474.58
Bosentan 147536-97-8 C27H29N5O6S 551.61
Sitaxsentan (sodium) 210421-74-2 C18H14ClN2NaO6S2 476.89
Bosentan (hydrate) 157212-55-0 C27H31N5O7S 569.63
11

Route of Synthesis

12

References

13

More Information

Macitentan

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