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Merck

SML2104

Ambrisentan

≥98% (HPLC), Endothelin ETA Receptor Antagonist, powder

Sinónimos:

(+)-(2S)-2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropanoic acid

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Fórmula empírica (notación de Hill):
C22H22N2O4
Número CAS:
Peso molecular:
378.42
NACRES:
NA.77
UNSPSC Code:
41121706
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Servicio técnico
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Nombre del producto

Ambrisentan, ≥98% (HPLC)

assay

≥98% (HPLC)

form

powder

optical activity

[α]/D +160 to +190°, c = 0.5 in methanol

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

CC1=CC(C)=NC(O[C@@H](C(C2=CC=CC=C2)(OC)C3=CC=CC=C3)C(O)=O)=N1

InChI

1S/C22H22N2O4/c1-15-14-16(2)24-21(23-15)28-19(20(25)26)22(27-3,17-10-6-4-7-11-17)18-12-8-5-9-13-18/h4-14,19H,1-3H3,(H,25,26)

InChI key

OUJTZYPIHDYQMC-UHFFFAOYSA-N

Biochem/physiol Actions

Ambrisentan is an endothelin receptor antagonist used in the treatment of pulmonary arterial hypertension (PAH). It is 200-fold selective for the the ETA receptor subtype with a Ki of 1 nM for ETA and a Ki of 195 nM for ETB.
Endothelin ETA Receptor Antagonist; Antihypertensive; Pulmonary Hypertension Treatment


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pictograms

Health hazard

signalword

Danger

hcodes

Hazard Classifications

Repr. 1A

Clase de almacenamiento

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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Belinda N Rivera-Lebron et al.
Therapeutic advances in respiratory disease, 11(6), 233-244 (2017-04-21)
Pulmonary arterial hypertension (PAH) is a progressive disease defined by an elevation in pulmonary arterial pressure that can lead to right heart failure and death. Ambrisentan is a selective endothelin receptor antagonist approved for the treatment of idiopathic, heritable PAH
Johanna Weiss et al.
European journal of pharmacology, 660(2-3), 298-304 (2011-04-20)
The safety and effectiveness of drugs used to treat chronic diseases critically depend on their propensity to interact with co-administered drugs. Induction of enzymes and drug transporters involved in the clearance and distribution of drugs may critically reduce exposure with
James A Angus et al.
European journal of pharmacology, 804, 111-116 (2017-03-17)
Endothelin receptor antagonists are approved for pulmonary arterial hypertension. Development of selective ET Human isolated pulmonary (i.d. 5.5mm) and human radial (i.d. 3.23mm) artery ring segments were mounted in organ baths for isometric force measurement. Single concentration-contraction curves to endothelin-1