CAS NO: | 136553-81-6 |
包装: | 500μg |
市场价: | 1271元 |
Cas No. | 136553-81-6 |
别名 | 环(D-ALPHA-天冬氨酰-L-脯氨酰-D-缬氨酰-L-亮氨酰-D-色氨酰) |
化学名 | 2-((3R,6S,9S,12S,17aS)-9-((1H-indol-3-yl)methyl)-6-isobutyl-3-isopropyl-1,4,7,10,13-pentaoxohexadecahydro-1H-pyrrolo[1,2-a][1,4,7,10,13]pentaazacyclopentadecin-12-yl)acetic acid |
Canonical SMILES | O=C([C@H]1N(C([C@H](CC(O)=O)NC([C@H](CC2=CNC3=CC=CC=C23)NC4=O)=O)=O)CCC1)N[C@@H](C(N[C@H]4CC(C)C)=O)C(C)C |
分子式 | C31H42N6O7 |
分子量 | 611 |
溶解度 | DMF: 1 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml,PBS (pH 7.2): slightly |
储存条件 | Desiccate at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | BQ-123 is a potent and selective antagonist of ETA endothelin receptor with Ki values of 1.4 and 1500 nM for ETA and ETB receptors, respectively. Endothelin receptor is a G protein-coupled receptor. ETA receptor increases intracellular-free Ca2+. Also, Activation of ETA receptor increases vasoconstriction and blood pressure. BQ-123 is a selective ETA receptor antagonist. In the ETA-expressing cells, BQ123 (10-6 M) inhibited endothelin-1 (ET-1) (10-6 M)-induced [Ca2+]i increase by 95% [1]. In rat vascular smooth muscle cells (VSMC), BQ-123 inhibited ET-1 receptor binding, cellular contraction, [Ca2+ ]i mobilization, [3H]thymidine incorporation, MAP kinase activation and MTT reduction induced by ET-1. However, BQ-123 didn’t inhibit angiotensin II (Ang II)- and arginine vasopressin (AVP)-induced increases in MAP kinase activity and [Ca2+]i mobilization [2]. In spontaneously hypertensive rats (SHR), renin hypertensive rats and normotensive rats, BQ-123 (16 nM/kg/min) reduced mean arterial pressure in a dose-dependent way in SHR. Also, BQ-123 lowered blood pressure in both renin hypertensive rats and normotensive rats [3]. In a kidney transplantation rat model with reperfusion injury, BQ-123 prevented reperfusion injury and inhibited the synthesis and release of ET-1,2 [4]. References: |