• Skip to primary navigation
  • Skip to main content
  • Skip to footer

LKT Labs

Biochemicals for Life Science Research

  • Products
    • New Products
    • Cancer Biology
    • Cardiovascular
    • Endocrine Signaling and Immunology
    • Metabolic and GI Pathology
    • Microbiology
    • Natural Products
    • Neuroscience
    • Peptides
    • Pharmaceutical Impurities and Derivatives
    • Stem Cell Modulators
  • Services
    • Custom Synthesis
    • Natural Product Isolation
    • Analytical Services
  • Int’l Distributors
  • Support
    • About LKT Labs
    • General Inquiry
    • Bulk Quote Request
    • Document Request
    • Technical Support
    • Catalog Request
    • Product Flyers
  • Contact Us
  • Cart
  • Login / Register
Macitentan

Macitentan

Product ID M0009
Cas No. 441798-33-0
Purity ≥99%
Product Unit SizeCostQuantityStock
1 mg $52.50 In stock
5 mg $112.60 In stock
25 mg $277.90 In stock
Bulk Quote

Quicklinks

  • Description
  • Product Info
  • Shipping and Storage
  • Downloads
  • References
  • Description
  • Product Info
  • Shipping and Storage
  • Downloads
  • References
  • Custom Order

Description

Macitentan is a dual endothelin receptor (ET-A/B)antagonist that displays antihypertensive, anti-fibrotic, and anticancer activity; this compound exhibits slower receptor dissociation kinetics than other endothelin receptor antagonists. Macitentan is currently used to treat pulmonary arterial hypertension, as clinical trials show that it decreases blood pressure and proteinuria and prevents right ventricle hypertrophy. In models of systemic sclerosis, macitentan slowed the fibrotic process. In other animal models, macitentan enhanced toxicity of a variety of other chemotherapeutics, increasing apoptosis in tumor cells and decreasing levels of phosphorylated VEGFR2, phosphorylated Akt, and MAPK.

Product Info

Cas No.

441798-33-0

Purity

≥99%

Formula

C19H20Br2N6O4S

Formula Wt.

588.27

IUPAC Name

5-(4-bromophenyl)-6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-N-(propylsulfamoyl)pyrimidin-4-amine

Synonym

ACT-064992, Actelion-1

Solubility

33mg/ml in DMSO and DMF

Appearance

White to off white powder

Shipping and Storage

Store Temp

Ambient

Ship Temp

Ambient

Downloads

MSDS

M0009 MSDS PDF

Info Sheet

M0009 Info Sheet PDF

References

Pulido T, Adzerikho I, Channick RN, et al. Macitentan and morbidity and mortality in pulmonary arterial hypertension. N Engl J Med. 2013 Aug 29;369(9):809-18. PMID: 23984728.

Corallo C, Pecetti G, Iglarz M, et al. Macitentan slows down the dermal fibrotic process in systemic sclerosis: in vitro findings. J Biol Regul Homeost Agents. 2013 Apr-Jun;27(2):455-62. PMID: 23830395.

Gatfield J, Mueller Grandjean C, Sasse T, et al. Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial smooth muscle cells. PLoS One. 2012;7(10):e47662. PMID: 23077657.

Kim SJ, Kim JS, Kim SW, et al. Antivascular therapy for multidrug-resistant ovarian tumors by macitentan, a dual endothelin receptor antagonist. Transl Oncol. 2012 Feb;5(1):39-47. PMID: 22348175.

Kim SJ, Kim JS, Kim SW, et al. Macitentan (ACT-064992), a tissue-targeting endothelin receptor antagonist, enhances therapeutic efficacy of paclitaxel by modulating survival pathways in orthotopic models of metastatic human ovarian cancer. Neoplasia. 2011 Feb;13(2):167-79. PMID: 21403842.

Iglarz M, Binkert C, Morrison K, et al. Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist. J Pharmacol Exp Ther. 2008 Dec;327(3):736-45. PMID: 18780830.

Custom Order

  • Size of single unit expressed as number (e.g. '500' in the case of 500 mg)
  • Total quantity of unit size desired (e.g. '10' in the case of 10 x 500 mg). If only one unit is desired, you may leave this blank.
  • This field is for validation purposes and should be left unchanged.

Related Products

  • M1678

    2-Methoxyestradiol

    Estradiol metabolite; microtubule depolymerizat...

    ≥98%
  • P4132

    PKI-402

    p110α PI3K and mTOR inhibitor.

    ≥98%
  • D1643

    Delta Sleep Inducing Peptide

    Peptide; GABA potentiator, NMDA negative allost...

    ≥95%
  • R3347

    Riluzole

    Benzothiazole; TRPC5 agonist, PTR1 inhibitor, v...

    ≥98%
  • M3310

    Miconazole Nitrate

    Imidazole; 14-α demethylase inhibitor, potenti...

    ≥98%
  • E7209

    Escitalopram Oxalate

    S-enantiomer of citalopram; SERT inhibitor.

    ≥99%
  • P0008

    Pituitary Adenylate Cyclase-activating Peptide (6-38), human/sheep/rat

    Endogenous peptide, involved in paracrine and a...

    ≥95%
  • L3454

    Lincomycin Hydrochloride Monohydrate

    Lincosamide; peptidyl transferase inhibitor, pr...

    ≥98%
  • C0253

    Candesartan

    AT1 inhibitor.

    ≥98%
  • A5061

    Ampalex

    Benzylpiperidine; AMPA potentiator.

    ≥98%
  • T2835

    6-Thioguanine

    Nucleotide (guanine) analog, prevents guanine s...

    ≥90%
  • H1794

    Hexamethonium Bromide Hydrate

    Non-depolarizing NMJ blocker; nAChR antagonist....

    ≥98%
  • N5770

    Norfloxacin Hydrochloride

    First generation fluoroquinolone antibiotic.

    ≥98%
  • L1782

    Levodopa

    Endogenous catecholamine precursor, also found ...

    ≥98%
  • R3586

    Rivastigmine Tartrate

    AChE and BChE inhibitor.

    ≥99%
  • M1879

    Metoprolol Tartrate

    β1-adrenergic antagonist.

    ≥98%
  • U698576

    Urolithin B

    Ellagic acid derivative produced by gut microfl...

    ≥99%
  • A1202

    Adapalene

    Tretinoin analog; RARα/β/γ agonist.

    ≥98%
  • K1679

    (+)-Ketanserin Tartrate

    5-HT2A and TRPV1 antagonist, potential α1-adre...

    ≥98%
  • B5871

    Bortezomib

    Proteasome inhibitor.

    ≥98%

Footer

  • Contact Us
  • About Us
  • Site Map
  • Terms and Conditions
LKT Laboratories, Inc.
545 Phalen Blvd.
St. Paul MN, 55130

Ph: (888)-558-5227
Fax: (888)-558-7329

©2025 LKT Laboratories, All Rights Reserved - Products for research use only