1. GPCR/G Protein
    Apoptosis
  2. Endothelin Receptor
    Apoptosis
  3. Macitentan

Macitentan (Synonyms: ACT-064992)

Cat. No.: HY-14184 Purity: 99.87%
Handling Instructions

Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).

For research use only. We do not sell to patients.

Macitentan Chemical Structure

Macitentan Chemical Structure

CAS No. : 441798-33-0

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Macitentan:

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Description

Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH)[1].

IC50 & Target

ETA/ETB[1]

In Vitro

Tube formation ability is restored when microvascular endothelial cells are preincubated with BOS or macitentan (ACT-064992), also reducing the expression of mesenchymal markers and restoring CD31 expression and the imbalance between VEGF-A and VEGF-A165b[1]. Macitentan inhibits OATP1B1-mediated uptake of atorvastatin and OATP1B3-mediated uptake of estrone-3-sulfate with IC50 ± SE values of 6.3 ± 0.7 and 11.8 ± 5.0 μM, respectively[3]. Treatment with macitentan or with ACT-132577 does not lead to intracellular accumulation of R123 in HeyA8-MDR, showing that these compounds are not P-gp inhibitors[4].

In Vivo

Macitentan (ACT-064992; 25 mg/kg/day, p.o.) prevents increased production of vasoactive and fibrogenic factors, NF-κB activation, structural and functional changes, and increases extracellular matrix protein production in type 2 diabetes in type 2 diabetes[2]. Macitentan (10 mg/kg, p.o.) coupled with once-per-week 5 mg/kg taxol, significantly reduces the weight (size) of HeyA8-MDR tumors in mice. Combination therapy with macitentan (10 or 50 mg/kg, but not 5 mg/kg) and taxol or macitentan (10 mg/kg) and cisplatinum significantly reduces the number of proliferating Ki-67-positive cells[4].

Clinical Trial
Molecular Weight

588.27

Formula

C₁₉H₂₀Br₂N₆O₄S

CAS No.

441798-33-0

SMILES

BrC1=CN=C(OCCOC2=C(C3=CC=C(Br)C=C3)C(NS(NCCC)(=O)=O)=NC=N2)N=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (84.99 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6999 mL 8.4995 mL 16.9990 mL
5 mM 0.3400 mL 1.6999 mL 3.3998 mL
10 mM 0.1700 mL 0.8499 mL 1.6999 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

Male db/db mice and age and sex-matched controls (27-32 g) are used for the assay. RandomLy selected diabetic animals are monitored for either 2 months or for 4 months after onset of diabetes. Groups (n=7/group) of the diabetic mice are subjected to oral macitentan treatment for the same period (25 mg/kg/day, food admix). The animals are monitored through assessment of body weight and blood glucose.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.87%

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Keywords:

MacitentanACT-064992ACT064992ACT 064992Endothelin ReceptorApoptosisorallynon-peptideETAETBendothelinidiopathicpulmonaryfibrosisarterialhypertensionInhibitorinhibitorinhibit

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