Embusartan - CAS 156001-18-2
Catalog number: 156001-18-2
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C25H24FN5O3
Molecular Weight:
461.49
COA:
Inquire
Targets:
Angiotensin Receptor
Description:
Embusartan, an oxopyridine derivative, has been found to be an angiotensin II receptor antagonist that was once studied against hypertension by Bayer.
Purity:
98%
Appearance:
Powder
Synonyms:
Embusartan; UNII-4MY73645XA; Embusartan [INN]; Bay 10-6734; Bay-10-6734; methyl 2-butyl-1-[[2-fluoro-4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-6-oxopyridine-4-carboxylate
Storage:
Store in a cool and dry place and at 0 - 4 °C for short term (days to weeks) or -20 °C for long term (months to years).
MSDS:
Inquire
Quality Standard:
In-house standard
Quantity:
Milligram-Grams
InChIKey:
LYVGOAYMIAQLHI-UHFFFAOYSA-N
InChI:
InChI=1S/C25H24FN5O3/c1-3-4-7-19-12-18(25(33)34-2)14-23(32)31(19)15-17-11-10-16(13-22(17)26)20-8-5-6-9-21(20)24-27-29-30-28-24/h5-6,8-14H,3-4,7,15H2,1-2H3,(H,27,28,29,30)
Canonical SMILES:
CCCCC1=CC(=CC(=O)N1CC2=C(C=C(C=C2)C3=CC=CC=C3C4=NNN=N4)F)C(=O)OC
1.Effects of BAY 10-6734 (Embusartan), a new angiotensin II type I receptor antagonist, on vascular smooth muscle cell growth.
Iouzalen L;Stepien O;Marche P J Pharmacol Exp Ther. 1999 Apr;289(1):181-7.
Angiotensin II (AII), an important hypertrophic factor in the cardiovascular system, exerts most of its known effects in vivo through the AII receptor type 1 (AT1) subclass of AII receptors. These receptors are also responsible for the growth-related effects of AII in cultured vascular smooth muscle cells (VSMCs). We presently investigated the effects of BAY 10-6734 (Embusartan), a new orally active AT1 antagonist, on VSMC growth and proliferation of cultured VSMCs isolated from the aortae of Wistar Kyoto rats and spontaneously hypertensive rats. BAY 10-6734 and losartan (considered as AT1 receptor antagonist of reference), as well as their respective active metabolites, were studied for their inhibition of: 1) [125I]AII binding to its receptors, 2) AII-induced DNA and protein synthesis (by measuring the incorporation of 5-bromo-2'-deoxyuridine and [3H]L-leucine, respectively), and 3) AII-induced variations in intracellular Ca2+ concentration, using cells labeled with Fura-2. All of the tested compounds inhibited the aforementioned parameters in a concentration-dependent manner. Half-maximal inhibitory concentration values indicated that BAY 10-6734 was significantly more potent than losartan and that spontaneously hypertensive rat-derived VSMCs were more sensitive than Wistar Kyoto rat-derived ones.
2.Long-term blockade of the angiotensin II receptor in renin transgenic rats, salt-loaded Dahl rats, and stroke-prone spontaneously hypertensive rats.
Stasch JP;Knorr A;Hirth-Dietrich C;Krämer T;Hübsch W;Dressel J;Fey P;Beuck M;Sander E;Frobel K;Kazda S Arzneimittelforschung. 1997 Sep;47(9):1016-23.
These studies were designed to investigate the protective effects of the new angiotensin II receptors antagonist BAY 10-6734 (6-n-butyl-4-methoxycarbonyl-2-oxo-1[(2'-(1H-tetrazol-5-yl) -3-fluorobiphenyl-4-yl)methyl] 1,2-dihydropyridine, CAS 156001-18-2) on haemodynamic, hormonal, renal, and structural parameters in renin transgenic rats (TGR(mRen2)27), salt-loaded Dahl S and R rats, and salt-loaded stroke-prone spontaneously hypertensive rats (SHR-SP) in long-term trials. Study 1: In SHR-SP the development of blood pressure, cardiac hypertrophy, and the deleterious effects of salt loading on kidney structure and kidney function was prevented by BAY 10-6734. Study 2: In salt-loaded Dahl S rats with a suppressed plasma renin activity treatment with BAY 10-6734 did not delay the increase in blood pressure but prevented cardiac hypertrophy and the increase in plasma ANP (Atrial natriuretic peptide). Study 3: TGR develop malignant hypertension associated with cardiac hypertrophy, elevated left-ventricular end-diastolic pressure and increased plasma ANP. After 6 weeks of treatment with BAY 10-6734 (30 mg/kg p.o. bid) cardiac pump function was improved and cardiac hypertrophy was reversed in this angiotension dependent form of hypertension.
3.Central nervous system blockade by peripheral administration of AT1 receptor blockers.
Wang JM;Tan J;Leenen FH J Cardiovasc Pharmacol. 2003 Apr;41(4):593-9.
After peripheral administration, AT(1) receptor blockers appear to be able to enter the brain and cause AT(1) receptor blockade in the central nervous system. In the current study, we investigated the effects of subcutaneous administration of embusartan versus losartan on inhibition of AT(1) receptor binding in rat brain by in vitro autoradiography. At 4 hours after single doses of 5, 30, or 100 mg/kg, both losartan and embusartan decreased iodine 125I Ang II binding dose dependently in brain structures that express AT(1) receptors both outside (e.g., organum vasculosum laminae terminalis) and within (e.g., paraventricular nucleus) the blood-brain barrier. At low doses, embusartan was twofold more potent than losartan inside but not outside the blood-brain barrier. After chronic treatment (30 mg/kg daily for 6 days), at 4 hours after the last dose, embusartan still caused more inhibition than losartan in the brain structures inside the blood-brain barrier. At 24 hours after the last dose, a modest, better inhibition for embusartan versus losartan remained: from 15% to 33% versus 10% to 24%, respectively. At 36 hours after the last dose, the inhibition for both blockers had almost completely disappeared inside the blood-brain barrier but persisted in, for example, the kidneys.
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CAS 156001-18-2 Embusartan

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