Top Suppliers:I want be here
Related CAS#:
177036-94-1 1007358-76-0
713516-99-5 1046116-27-1
1386915-48-5 1189479-60-4
1392210-85-3 1106685-66-8
1240470-84-1 1106685-84-0
1158522-08-7 940364-43-2
134104-43-1 131615-57-1
6906-52-1 930439-75-1
1018584-77-4 1375289-11-4
849349-65-1 127437-46-1

177036-94-1

177036-94-1 structure
177036-94-1 structure
Name (2S)-2-(4,6-dimethylpyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid
Synonyms Letairis
(2S)-2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropanoic acid
(S)-2-(4,6-Dimethylpyrimidin-2-yloxy)-3-methoxy-3,3-diphenylpropanoic acid
ambrisentan
Benzenepropanoic acid, α-[(4,6-dimethyl-2-pyrimidinyl)oxy]-β-methoxy-β-phenyl-, (αS)-
(2S)-2-[(4,6-Dimethyl-2-pyrimidinyl)oxy]-3-methoxy-3,3-diphenylpropanoic acid
UNII-HW6NV07QEC
Description Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
Related Catalog
Target

ETA receptor[1]

In Vitro Ambrisentan is an endothelin type A receptor antagonist[1]. Ambrisentan induces Nrf2 activation. Endothelial permeability increased in BMEC monolayers at 24 h of hypoxia exposure and compared to vehicle control, Ambrisentan attenuates hypoxia-induced BMEC leak. These results are reversed when prior to treatment BMEC are transfected with siRNA against Nrf2[2].
In Vivo In the Ambrisentan group, hepatic hydroxyproline content is significantly lower than in the control group (18.0 μg/g±6.1 μg/g vs 33.9 μg/g±13.5 μg/g liver, respectively, P=0.014). Hepatic fibrosis estimated by Sirius red staining and areas positive for α-smooth muscle actin, indicative of activated hepatic stellate cells, are also significantly lower in the Ambrisentan group (0.46%±0.18% vs 1.11%±0.28%, respectively, P=0.0003; and 0.12%±0.08% vs 0.25%±0.11%, respectively, P=0.047). Moreover, hepatic RNA expression levels of procollagen-1 and tissue inhibitor of metalloproteinase-1 (TIMP-1) are significantly lower by 60% and 45%, respectively, in the Ambrisentan group. Inflammation, steatosis, and endothelin-related mRNA expression in the liver are not significantly different between the groups. Ambrisentan attenuates the progression of hepatic fibrosis by inhibiting hepatic stellate cell activation and reducing procollagen-1 and TIMP-1 gene expression. Ambrisentan did not affect inflammation or steatosis[1].
Cell Assay Unless otherwise stated, for each BMEC experiment cells are randomly divided into 4 groups: (1) normoxia vehicle control (Nx-CTRL); (2) normoxia-treated; (3) hypoxia (24 h) control (Hx-CTRL) and (4) hypoxia (24 h) treated. As previously described, Nrf2 activators are added 24 h prior to any hypoxic exposures. Cell treatments are; Protandim (100 μg/mL), methazolamide (125 μg/mL, nifedipine (7 μg/mL) or Ambrisentan (40 μg/mL). In addition, some cells are treated with Nrf2 siRNA. In these experiments, siRNA is added 24 h prior to drug treatments. The rationale for 24 h hypoxia exposure for BMEC is to ensure that cells remained transfected with siRNA for the pre-treatment of drugs (24 h in normoxia) and during the 24 h hypoxia exposure. Data is collected from at least three separate cell culture preparations on three separate days (n=9)[2].
Animal Admin Mice[1] A total of 13 male FLS-ob/ob mice (age, 8 wk; body weight, 42.88 g±1.74 g) are used. At the age of 12 wk, male FLS-ob/ob mice are randomly assigned to the Ambrisentan (n=8) or control (n= 5) group. Intragastric gavage administration is carried out in conscious animals with an appropriately sized gastric tube. Ambrisentan (2.5 mg/kg per day) is orally administered every afternoon for 4 wk as a bolus through a gastric tube. Water is administered to the control group. At week 4, animals are fasted for 4 h and tail vein blood is drawn and subjected to blood glucose determination. Animals are killed by pentobarbital anesthesia injection after 4 wk and blood is collected from the right ventricle. Plasma samples are frozen and stored at -80°C Liver and visceral fat are then weighed, snap-frozen in liquid nitrogen, and stored at -80°C. Additional liver specimens are fixed in 10% buffered formalin and embedded in paraffin for histological analysis.
References

[1]. Okamoto T, et al. Antifibrotic effects of Ambrisentan, an endothelin-A receptor antagonist, in a non-alcoholic steatohepatitis mouse model. World J Hepatol. 2016 Aug 8;8(22):933-41.

[2]. Lisk C, et al. Nrf2 activation: a potential strategy for the prevention of acute mountain sickness. Free Radic Biol Med. 2013 Oct;63:264-73.
Density 1.228g/cm3
Boiling Point 551.1ºC at 760mmHg
Melting Point >150°C (dec.)
Molecular Formula C22H22N2O4
Molecular Weight 378.42100
Flash Point 287.1ºC
Exact Mass 378.15800
PSA 81.54000
LogP 3.51560
Vapour Pressure 5.56E-13mmHg at 25°C
Index of Refraction 1.593
Storage condition -20°C Freezer
Risk Phrases 62/63
Safety Phrases 53-36/37/39-45
RTECS UA2459660
HS Code 2933599090
HS Code 2933599090
Summary 2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Chemsrc provides CAS#:177036-94-1 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 177036-94-1 | Chemsrc address: https://m.chemsrc.com/en/baike/453217.html

Home | MSDS/SDS Database Search | Journals | Product Classification | Biologically Active Compounds | Selling Leads | About Us | Disclaimer

Copyright © 2024 ChemSrc All Rights Reserved