Avosentan - CAS 290815-26-8
Catalog number: 290815-26-8
Category: Inhibitor
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Molecular Formula:
C23H21N5O5S
Molecular Weight:
479.51
COA:
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Targets:
Endothelin Receptor
Description:
Avosentan, also known as SPP301, R-639, and RO 67-0565, is a potent and selective endothelin receptor(ETA receptor) antagonist.
Purity:
95%
Appearance:
Solid powder
Synonyms:
N-[6-methoxy-5-(2-methoxyphenoxy)-2-pyridin-4-ylpyrimidin-4-yl]-5-methylpyridine-2-sulfonamide;Avosentan;290815-26-8;UNII-L94KSX715K;SPP301; SPP301; SPP301; RO 67-0565; RO-67-0565; RO67-0565; R-639; Avosentan
Solubility:
Soluble in DMSO
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -41℃ for long term (months to years).
MSDS:
Inquire
Shelf Life:
2 years
Quantity:
Data not available, please inquire.
Boiling Point:
575.472ºC at 760 mmHg
Density:
1.364 g/cm3
InChIKey:
YBWLTKFZAOSWSM-UHFFFAOYSA-N
InChI:
1S/C23H21N5O5S/c1-15-8-9-19(25-14-15)34(29,30)28-22-20(33-18-7-5-4-6-17(18)31-2)23(32-3)27-21(26-22)16-10-12-24-13-11-16/h4-14H,1-3H3,(H,26,27,28)
Canonical SMILES:
CC1=CN=C(C=C1)S(=O)(=O)NC2=C(C(=NC(=N2)C3=CC=NC=C3)OC)OC4=CC=CC=C4OC
1.Avosentan is protective in hypertensive nephropathy at doses not causing fluid retention.
Baltatu OC1, Zaugg CE2, Schumacher C3, Louie P3, Campos LA4, Bader M5. Pharmacol Res. 2014 Feb;80:9-13. doi: 10.1016/j.phrs.2013.12.003. Epub 2013 Dec 22.
Multiple studies indicate that endothelin antagonism may have a protective effect for chronic kidney disease. Despite that, clinical studies using avosentan have been halted due to adverse effects including fluid overload. Therefore, we aimed at investigating whether avosentan may have protective effects against hypertensive nephropathy at doses below those inducing fluid-retention. We used double transgenic rats (dTGR), overexpressing both the human renin and angiotensinogen gene, which develop malignant hypertension. Effects of avosentan alone or in combination with low-dose of valsartan (angiotensin AT1 receptor antagonist) on end-organ damage were studied. Avosentan induced a decrease of diuresis (18.3%) with a consequent decrease in hematocrit (8.3%) only at the highest dose investigated (100mg/kg). Treatment with the combination of avosentan and valsartan (10 and 0.1mg/kg, once daily by gavage, respectively) decreased albuminuria to a greater extent than each compound given alone (avosentan: 19.
2.Antidiuretic effects of the endothelin receptor antagonist avosentan.
Baltatu OC1, Iliescu R, Zaugg CE, Reckelhoff JF, Louie P, Schumacher C, Campos LA. Front Physiol. 2012 Apr 18;3:103. doi: 10.3389/fphys.2012.00103. eCollection 2012.
Several clinical studies have investigated the potential benefits of endothelin receptor antagonism in chronic pathologies such as diabetic kidney disease. However, fluid retention and edema have been identified as major side effects of endothelin receptor antagonists. In the present study we hypothesized that avosentan which was described as a predominant ET(A) receptor antagonist would produce fluid retention at high concentrations where non-specific blockade of ET(B) receptors may occur. Incremental doses of the predominant ET(A) receptor antagonist SPP301 (0.003; 0.03; 3 mg/kg) were administered intravenously to anesthetized Sprague-Dawley rats undergoing saline diuresis. Diuresis, glomerular filtration rate, and blood pressure (BP) were monitored. SPP301 decreased urine output (5.6; 34.8; 58.8% decrease from vehicle) and fractional excretion of water (5.7; 31.7; 56.4% decrease from vehicle) in a concentration-dependent manner. Glomerular filtration rate was unchanged while BP was reduced by 10 mmHg only by the highest dose of SPP301.
3.Effect of avosentan (SPP-301) in porcine ciliary arteries.
Konieczka K1, Meyer P, Schoetzau A, Neutzner A, Mozaffarieh M, Flammer J. Curr Eye Res. 2011 Feb;36(2):118-24. doi: 10.3109/02713683.2010.529982.
PURPOSE: To investigate the vasoactive effect of ET(A)-endothelin receptor antagonists avosentan (SPP-301) and BQ-123 in isolated porcine ciliary arteries with and without endothelium. To investigate the effect of avosentan on the endothelin-1 induced contractions in comparison with BQ-123 and BQ-788 (ET(B)-endothelin receptor antagonist) in isolated porcine ciliary arteries with and without endothelium.
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CAS 290815-26-8 Avosentan

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