Enrasentan - CAS 167256-08-8
Catalog number: 167256-08-8
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
Molecular Weight:
Endothelin Receptor
Enrasentan, an indene derivative, has been found to be an endothelin receptor antagonist that was once studied in reperfusion injury and heart failure therapy.
Enrasentan; SB-217242; UNII-QG16H8A6ZH; SB 217242; SB217242; CHEMBL431651; (1S,2R,3S)-1-(1,3-benzodioxol-5-yl)-3-[2-(2-hydroxyethoxy)-4-methoxyphenyl]-5-propoxy-2,3-dihydro-1H-indene-2-carboxylic acid
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).
Quality Standard:
In-house standard
Canonical SMILES:
1.Elevated pressure selectively blunts flow-evoked vasodilatation in rat mesenteric small arteries.
Christensen FH;Hansen T;Stankevicius E;Buus NH;Simonsen U Br J Pharmacol. 2007 Jan;150(1):80-7. Epub 2006 Nov 27.
BACKGROUND AND PURPOSE: ;The present study investigated mechanisms underlying impaired endothelium-dependent vasodilatation elicited by elevating the intraluminal pressure in rat mesenteric small arteries.;EXPERIMENTAL APPROACH: ;Arterial segments (internal diameter 316+/-2 microm, n=86) were mounted in a pressure myograph. The effect of elevating pressure from 50 to 120 mmHg for 1 h before resetting it to 50 mmHg was studied on endothelium-dependent vasodilatation.;KEY RESULTS: ;In arteries constricted with U46619 in the presence of indomethacin, shear stress generated by flow, evoked vasodilatation that was abolished by an inhibitor of nitric oxide (NO) synthase, asymmetric dimethylarginine (1 mM), whereas acetylcholine-induced vasodilatation was unchanged. After elevation of intraluminal pressure for 1 h and then resetting it to 50 mmHg, vasodilatation induced by shear stress and the NO donor, S-nitrosopenicillamine was inhibited, while vasodilatation induced by a guanylyl cyclase activator, BAY 412272, and acetylcholine was unaltered. Superoxide levels sensitive to polyethylene glycol superoxide dismutase were increased in segments exposed to elevated pressure. A superoxide scavenger, tempol (300 microM), a general endothelin receptor antagonist, SB 217242 and the selective ET(A) receptor antagonist, BQ 123 preserved shear stress-evoked vasodilatation.
2.Enrasentan improves survival, limits left ventricular remodeling, and preserves myocardial performance in hypertensive cardiac hypertrophy and dysfunction.
Willette RN;Anderson KM;Nelson AH;Olzinski AR;Woods T;Coatney RW;Aiyar N;Ohlstein EH;Barone FC J Cardiovasc Pharmacol. 2001 Oct;38(4):606-17.
Evidence suggests that endothelin receptor antagonists may have therapeutic potential for the chronic treatment of heart failure. In the current study, the effects of an orally active mixed endothelin-A/endothelin-B (ETA /ETB ) receptor antagonist (enrasentan) were assessed in a model of cardiac hypertrophy and dysfunction (spontaneously hypertensive stroke prone rats) maintained on a high-salt/high-fat diet. Echocardiography was used to quantify cardiac performance and left ventricular dimensions. Enrasentan (1,200 and 2,400 parts per million in the high-salt/high-fat diet) had no significant effects on body weight and systolic blood pressure. However, increases in heart rate were not observed in the enrasentan-treated groups at 12 weeks (p < 0.05). Enrasentan-treated groups exhibited significantly improved survival (90-95% vs. 30% [control rats] at 18 weeks; p < 0.001). Enrasentan treatments also increased stroke volume (at 8, 12, and 16 weeks) and cardiac index (at 8 and 16 weeks) 33-50% and 45-63%, respectively. Enrasentan treatments reduced the relative wall thickness (14-27% at 8 and 12 weeks), ratio of left ventricular mass to body weight (20% at 12 weeks), and ratio of terminal heart weight to body weight (16-23%, p < 0.
3.Comparison of the dual receptor endothelin antagonist enrasentan with enalapril in asymptomatic left ventricular systolic dysfunction: a cardiovascular magnetic resonance study.
Prasad SK;Dargie HJ;Smith GC;Barlow MM;Grothues F;Groenning BA;Cleland JG;Pennell DJ Heart. 2006 Jun;92(6):798-803. Epub 2005 Dec 9.
OBJECTIVE: ;To compare the effect of the dual endothelin A/B receptor antagonist enrasentan with enalapril on left ventricular (LV) remodelling.;METHODS: ;Multicentre, randomised, double blind, parallel group study of 72 asymptomatic patients with LV dysfunction. Patients received enrasentan (60-90 mg/day) or enalapril (10-20 mg/day). The primary end point was the change in LV end diastolic volume index (EDVI) after six months' treatment.;RESULTS: ;LV EDVI increased with enrasentan but decreased with enalapril (3.9 (1.8) v -3.4 (1.4) ml/m2, p = 0.001). Enrasentan increased resting cardiac index compared with enalapril (0.11 (0.07) v -0.10 (0.07) l/m2, p = 0.04), as well as LV mass index (0.67 (1.6) v -3.6 (1.6) g/m2, p = 0.04). Other variables were comparable between groups. Enalapril lowered brain natriuretic peptide more than enrasentan (-19.3 (9.4) v -5.8 (6.9) pg/ml, p = 0.005). Noradrenaline (norepinephrine) (p = 0.02) increased more with enrasentan than with enalapril. Enrasentan was associated with more serious adverse events compared with enalapril (six (16.7%) patients v one (2.8%), p = 0.02); the rate of progression of heart failure did not differ.;CONCLUSION: ;In asymptomatic patients with LV dysfunction, LV EDVI increased over six months with enrasentan compared with enalapril treatment, with adverse neurohormonal effects.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Endothelin Receptor Products

CAS 1103522-45-7 N-Despropyl-macitentan

(CAS: 1103522-45-7)

N-Despropyl-macitentan, an active metabolite of Macitentan, is a dual ET receptor antagonist with longer half-life than Macitentan. It has been proved to be eff...

CAS 171714-84-4 Darusentan

(CAS: 171714-84-4)

Darusentan is a selective endothelin-1 receptor A inhibitor. Darusentan is identified as the treatment of congestive heart failure, hypertension and cancers. It...

CAS 169545-27-1 IRL-2500

(CAS: 169545-27-1)

IRL-2500, an indol derivative, has been found to be an endothelin B receptor antagonist that was once studied in hypertension.

CAS 180384-56-9 Clazosentan

(CAS: 180384-56-9)

Clazosentan, also called as AXV 034, Ro 61-1790 or VML 588, a novel endothelin A antagonist, improves cerebral blood flow and behavior after traumatic brain inj...

CAS 210891-04-6 Edonentan

(CAS: 210891-04-6)

Edonentan, also known as BMS-207940, is a very potent and selective ETA endothelin receptor antagonist (Ki= 10 pM) that shows 80000-fold selective for ETA vs ET...

CAS 162256-50-0 CI 1020

CI 1020
(CAS: 162256-50-0)

CI 1020 has been found to be a novel endothelin-A receptor antagonist and could be used as an antihypertensive agent.

CAS 186497-07-4 Zibotentan

(CAS: 186497-07-4)

Zibotentan is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).

CAS 142375-60-8 FR 139317

FR 139317
(CAS: 142375-60-8)

FR 139317 is a selective Endothelin A receptor antagonist originated by Fujisawa. (Ki values are 1 nM and 7.3 μM at ETA and ETB subtypes respectively). No devel...

Chemical Structure

CAS 167256-08-8 Enrasentan

Quick Inquiry

Verification code

Featured Items