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Macitentan

Cat. No. M2205
Macitentan Structure
Synonym:

ACT-064992

Size Price Availability Quantity
5mg USD 147 In stock
10mg USD 270 In stock
50mg USD 870 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Macitentan (ACT-064992) is a tissue-targeting dual ET(A)/ET(B) endothelin (ET) receptor antagonist designed for tissue targeting. Macitentan inhibited ET-1-induced contractions in isolated endothelium-denuded rat aorta (ET(A) receptors) and sarafotoxin S6c-induced contractions in isolated rat trachea (ET(B) receptors). In diabetic rats, chronic administration of macitentan decreased blood pressure and proteinuria and prevented end-organ damage. Treatment with macitentan enhanced the cytotoxicity mediated by paclitaxel as measured by the degree of apoptosis in tumor cells and tumor-associated endothelial cells. A Phase III clinical trial of macitentan was successfully completed in 2012.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 588.27
Formula C19H20Br2N6O4S
CAS Number 441798-33-0
Purity >99%
Solubility DMSO 80 mg/mL
Storage at -20°C
References

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.
Kim SJ, et al. Neoplasia. 2011 Feb;13(2):167-79. PMID: 21403842.

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

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Macitentan, ACT-064992 supplier, Endothelin Receptor, inhibitors

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