441798-33-0 Macitentan AKSci J96081
 
 
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  J96081    
Macitentan
, 95%
 
ACT064992




IDENTITY
CAS Number:441798-33-0
MDL Number:MFCD17167076
MF:C19H20Br2N6O4S
MW:588.27
SPECIFICATIONS & PROPERTIES
Min. Purity Spec:95%
Physical Form (at 20°C):Solid
Melting Point:135-138°C
Long-Term Storage:Store long-term at -20°C
DOT/IATA TRANSPORT INFORMATION
Not hazardous material

BIOLOGICAL INFO
Solubility:DMSO
Application(s):Endothelin ETA and ETB receptor antagonist

REVIEW

 Macitentan is an orally active, non-peptide, dual ETA/ETB (endothelin) receptor antagonist with IC50 of 0.5 nM/391 nM.

REFERENCES
[1]Kim SJ, Kim JS, Kim SW, Yun SJ, He J, Brantley E, Fan D, Strickner P, Lehembre F, Regenass U, Fidler IJ. Antivascular therapy for multidrug-resistant ovarian tumors by macitentan, a dual endothelin receptor antagonist. Transl Oncol. 2012 Feb;5(1):39-47.
[2] Bruderer S, Aänismaa P, Homery MC, Häusler S, Landskroner K, Sidharta PN, Treiber A, Dingemanse J. Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissue-targeting dual endothelin receptor antagonist. AAPS J. 2012 Mar;14(1):68-78.
[3] Bruderer S, Hopfgartner G, Seiberling M, Wank J, Sidharta PN, Treiber A, Dingemanse J. Absorption, distribution, metabolism, and excretion of macitentan, a dual endothelin receptor antagonist, in humans. Xenobiotica. 2012 Sep;42(9):901-10.
[4] Bolli MH, Boss C, Binkert C, Buchmann S, Bur D, Hess P, Iglarz M, Meyer S, Rein J, Rey M, Treiber A, Clozel M, Fischli W, Weller T. The Discovery of N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an Orally Active, Potent Dual Endothelin Receptor Antagonist. J Med Chem. 2012 Aug 16.

GLOBALLY HARMONIZED SYSTEM (GHS)

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501


Current as of April 19, 2024


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⚠️
All products are for research and development use only, not for any other uses, and must be handled by technically-qualified persons.

These products are explicitly not intended to be used in foods and/or cosmetics and/or drugs (human and veterinary) and/or consumer products and/or biocides and/or pesticides of any kind unless explicitly stated otherwise.

Products are not sold to individuals. We do not ship to residential addresses. Consumer orders will be cancelled without notice.

New customers undergo an internal onboarding process. As part of this process, new customers may be asked for more information. Additional restrictions may apply.



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