Macitentan

SKU: orb1305317

Description

Macitentan (ACT-064992) is a dual endothelin receptor antagonist employed in pulmonary arterial hypertension (PAH) research. It is widely used in both in vitro binding assays and in vivo animal models to study endothelin signaling pathways and evaluate potential therapeutic interventions.

Research Area

Cell Biology, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	441798-33-0
MW	588.27
Purity	99.88%
Formula	C₁₉H₂₀Br₂N₆O₄S
SMILES	N(S(NCCC)(=O)=O)C=1C(=C(OCCOC=2N=CC(Br)=CN2)N=CN1)C3=CC=C(Br)C=C3
Target	Endothelin Receptor,Apoptosis
Solubility	DMSO:93 mg/mL (158.09 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (5.61 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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Target IC50	ETA:0.5 nM\|ETB:391 nM
In Vivo	In primary human lung smooth muscle cells (IC50=1 nM), Macitentan inhibits the increase of intracellular calcium ions induced by ET-1. Additionally, Macitentan suppresses ET-1-induced contraction in isolated rat aortic rings. Furthermore, in isolated rat tracheal rings, Macitentan inhibits contraction induced by S6c. Read more...
In Vitro	In DOCA-salt-induced hypertensive rats, Macitentan (10 mg/kg) demonstrated a dose-dependent reduction in mean arterial blood pressure. Similarly, in a model of pulmonary arterial hypertension using monocrotaline-treated rats, oral administration of Macitentan (30 mg/kg/day) dose-dependently prevented the development of pulmonary arterial hypertension and right ventricular hypertrophy. Additionally, in type 2 diabetic db/db mice, oral Macitentan (25 mg/kg/day) reduced mRNA expression while concurrently enhancing NF-κB activation. Read more...

Storage & Handling

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Storage	store at low temperature,keep away from direct sunlight,keep away from moisture \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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arterial, Apoptosis, ACT064992, ACT-064992, ACT 064992, Inhibitor, hypertension, idiopathic, endothelin, Endothelin Receptor, EndothelinReceptor, ET-B, ETB, ET-A, ETA, fibrosis, inhibit, non-peptide, orally, Macitentan, pulmonary

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Compound Identifiers

PubChem CID

16004692 ↗

Key Properties

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No computed properties available.

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Macitentan (orb1305317)

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CAS Number:	556797-16-1
MW:	587.29
Formula:	C₂₀H₂₁Br₂N₅O₄S

MW:	550.22
Formula:	C₁₆H₁₀D₄Br₂N₆O₄S

MW:	578.27
Formula:	C₁₈H₁₄D₄Br₂N₆O₄S

Purity:	96.51%
CAS Number:	1258428-05-5
MW:	592.3
Formula:	C₁₉H₂₀Br₂N₆O₄S

Purity:	>98% (HPLC)
CAS Number:	441798-33-0
MW:	588.27
Formula:	C₁₉H₂₀Br₂N₆O₄S

Macitentan

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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Macitentan (orb1305317)

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