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Merck
CN

SML2104

Ambrisentan

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

别名:

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

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关于此项目

经验公式(希尔记法):
C22H22N2O4
化学文摘社编号:
分子量:
378.42
NACRES:
NA.77
UNSPSC Code:
41121706
MDL number:
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产品名称

Ambrisentan, ≥98% (HPLC)

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)

SMILES string

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

InChI key

OUJTZYPIHDYQMC-UHFFFAOYSA-N

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

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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

pictograms

Health hazard

signalword

Danger

hcodes

Hazard Classifications

Repr. 1A

存储类别

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

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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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
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
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
Sanah M Nkadimeng et al.
Scientific reports, 10(1), 22314-22314 (2020-12-20)
Prevalence of major depression in people with chronic heart failure is higher than in normal populations. Depression in heart failure has become a major issue. Psilocybin-containing mushrooms commonly known as magic mushrooms, have been used since ancient times for their
Ilenia Masi et al.
Cell reports, 34(9), 108800-108800 (2021-03-04)
Cancer cells use actin-based membrane protrusions, invadopodia, to degrade stroma and invade. In serous ovarian cancer (SOC), the endothelin A receptor (ETAR) drives invadopodia by a not fully explored coordinated function of β-arrestin1 (β-arr1). Here, we report that β-arr1 links

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