Macitentan (ACT 064992) - Moligand™, 10mM in DMSO , Endothelin receptor, ET-A/ET-B antagonist, CAS No.441798-33-0, Endothelin receptor, ET-A/ET-B antagonist

CAS: 441798-33-0 Cat. No.: M409076 Summenformel: C₁₉H₂₀Br₂N₆O₄S Molekulargewicht: 588.27 EG-Nummer: 810-007-8

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Sulfamide, N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propyl-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Information

Macitentan (ACT 064992) Macitentan (ACT 064992) is an orally active, non-peptide, dual ETA/ETB (endothelin) receptor antagonist with IC50 of 0.5 nM/391 nM.
In vitro

Macitentan achieves full inhibition of intracellular calcium increase induced by ET-1 on primary human pulmonary smooth muscle cells with approximate IC50 of 1 nM. Macitentan inhibits ET-1-induced contractions on isolated rat aortic rings or S6c-induced contractions on isolated rat tracheal rings with pA₂ of 7.6 and 5.9, respectively.

In vivo

Macitentan administered to normotensive rats, increases plasma ET-1 concentration, which occurred at a 10-fold lower dose than with bosentan. Macitentan dose-dependently decreases mean arterial blood pressure in hypertensive DOCA-salt rats with a maximal effect of -26 mm Hg at a dose of 10 mg/kg and a ED50 of 1mg/kg. At the maximal effective dose, the duration of the blood pressure response to Macitentan is approximately 40 hr. Macitentan orally administrated dose-dependently preventes the development of pulmonary hypertension and the development of right ventricle hypertrophy with a maximal efficacy of 30 mg/kg/day in monocrotaline rat model of pulmonary hypertension. Chronic oral administration of Macitentan at 30 mg/kg/day significantly improves the 42-day survival in monocrotaline rats (83 vs 50% survival in macitentan vs vehicle; 66% reduction of mortality at 42 days). Macitentan (30 mg/kg/day) treated for 24 h partially prevents the development of renal vasoconstriction and increases renal blood flow in streptozotocin-induced diabetic rat model. Macitentan increases glomerular filtration rate and decreases filtration fraction, and attenuates vascular and tubulo-interstitial lesions and also glomerular damage. Macitentan (25 mg/kg/day, p.o.) attenuates the increase of renal, cardiac and retinal ET-1, TGF-β1, VEGF, FN, EDB⁺FN, collagenα-I(IV) mRNA expression along with increased FN, collagen protein and NF-κB activation induced by type 2 diabetes in db/db mice. Macitentan also ameliorates mesangial expansion, cardiac dysfunction and the increased expression of ANP and BNP in these diabetic mice. Macitentan (100mg/kg) treatment combined with paclitaxel (5 mg/kg) reduced tumor incidence (5/9 vs 9/9 of paclitaxel along) and further reduces tumor weight (median [range]: 0.1 vs 0.4 g of paclitaxel along) and incidences of ascites (0/9 vs 4/9 of paclitaxel along) in SKOV3ip1 ovarian cancer model when compared with paclitaxel alone. Macitentan plus paclitaxel inhibits the phosphorylation of ETRs and suppresses the survival pathways of tumor cells by decreasing the levels of pVEGFR2, pAkt, and pMAPK. Macitentan enhances effects of paclitaxel on tumor cells dividing (Brud⁺ cells: 18.5 vs 30.8 of paclitaxel along) and apoptosis (TUNEL⁺ cells: 195 vs 150 of paclitaxel along).
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥97%

Specifications

Synonyme

Sulfamide, N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propyl-

Spezifikationen & Reinheit

Moligand™, 10mM in DMSO

Biochemische und physiologische Mechanismen

Macitentan (ACT 064992) is an orally active, non-peptide, dual ETA/ETB (endothelin) receptor antagonist with IC50 of 0.5 nM/391 nM.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

ANTAGONIST

Mechanismus der Wirkung

Endothelin receptor, ET-A/ET-B antagonist

Produkteigenschaften

• ALogP: 3.7

Namen und Kennungen

• Isomere SMILES: CCCNS(=O)(=O)NC1=C(C(=NC=N1)OCCOC2=NC=C(C=N2)Br)C3=CC=C(C=C3)Br
• Molekulargewicht: 588.27
• Reaxy-Rn: 11340634
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11340634&ln=

Zugehörige Ziele (menschlich)

EDNRA Tclin Endothelin-1 receptor (4 Activities)

Discover Target: EDNRA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EDNRB Tclin Endothelin receptor type B (1 Activities)

Discover Target: EDNRB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Häufig gestellte Fragen

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 441798-33-0, the molecular formula is C19H20Br2N6O4S, and the molecular weight is 588.27 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.