Darusentan

An ETA receptor antagonist

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库存: 现货

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5mg

￥1412.00

1130.00

- +
10mg

￥2400.00

1920.00

- +
50mg

￥7012.00

5610.00

- +
100mg

￥11875.00

9500.00

- +
200mg

￥0.00

0.00

- +
500mg

￥0.00

0.00

- +

已选 0 种 0 瓶

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货号: ajce55864
CAS: 171714-84-4
别名: 达卢生坦,Lu-135252
分子式: C22H22N2O6
分子量: 410.42
纯度: >98%
溶解度: DMSO: ≥ 125 mg/mL (304.57 mM); Water: < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

Darusentan is an endothelin type A (ET_A) receptor antagonist (K_i = 13 nM in rat aortic vascular smooth muscle cells).¹ It inhibits contractions induced by human endothelin-1 in isolated rat aortic rings and mesenteric microvessels with pA₂ values of 8.1 and 7.97, respectively. Darusentan (50 mg/kg) decreases systolic blood pressure in DOCA-salt hypertensive rats, as well as reduces mean arterial pressure (MAP) and left ventricular developed pressure (LVDP) in normotensive pigs when administered at doses of 1 and 5 mg/kg.^2,3 It reduces myocardial infarct size as a percentage of the area at risk in a porcine model of ischemia-reperfusion injury induced by ligation of the left anterior descending (LAD) coronary artery.³

1.Liang, F., Glascock, C.B., Schafer, D.L., et al.Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteriesCan. J. Physiol. Pharmacol.88(8)840-849(2010) 2.Schiffrin, E.L., Turgeon, A., and Deng, L.Y.Effect of chronic ETA-selective endothelin receptor antagonism on blood pressure in experimental and genetic hypertension in ratsBr. J. Pharmacol.121(5)935-940(1997) 3.Gonon, A.T., Wang, Q.D., Shimizu, M., et al.The novel non-peptide selective endothelin A receptor antagonist LU 135 252 protects against myocardial ischaemic and reperfusion injury in the pigActa Physiol. Scand.163(2)131-137(1998)