| CAS NO: | 136553-81-6 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| Physical Appearance | White lyophilised solid |
| Storage | Desiccate at -20°C |
| M.Wt | 611 |
| Cas No. | 136553-81-6 |
| Formula | C31H42N6O7 |
| Solubility | Soluble to 0.40 mg/ml in sterile water |
| Chemical Name | 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
BQ-123是一种强效的和选择性的ETA内皮素受体拮抗剂,作用于ETA和ETB受体的Ki值分别为1.4和1500 nM.
内皮素受体是一种G蛋白偶联受体.ETA受体增加细胞内游离Ca2+.另外,ETA受体的激活增加血管收缩和血压.
BQ-123是一种选择性的ETA受体拮抗剂.在表达ETA的细胞中,BQ 123(10-6 M)抑制内皮素-1(ET-1)(10-6 M)诱导的[Ca2 +] i增加达95%[1].在大鼠血管平滑肌细胞(VSMC)中,BQ-123抑制ET-1诱导的ET-1受体结合\细胞收缩\[Ca2 +]i动员\[3H]胸苷掺入\MAP激酶激活和MTT还原.然而,BQ-123不抑制血管紧张素II(ANG II)和精氨酸加压素(AVP)诱导的MAP激酶活性及[Ca2 +]i动员的增加[2].
在自发性高血压大鼠(SHR)\肾素高血压大鼠和正常血压大鼠中,BQ-123(16 nM/kg/min)剂量依赖性地降低SHR中的平均动脉压.此外,BQ-123降低肾素高血压大鼠和正常血压大鼠血压[3].在再灌注损伤肾脏移植大鼠模型中,BQ-123防止再灌注损伤并抑制ET-1,2的合成和释放[4].
参考文献：
[1]. Sakamoto A, Yanagisawa M, Sawamura T, et al. Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonist and endothelinB-selective agonists. J Biol Chem, 1993, 268(12): 8547-8553.
[2]. Guo X, Okada K, Fujita N, et al. Inhibitory effect of BQ-123 on endothelin-1-stimulated mitogen-activated protein kinase and cell growth of rat vascular smooth muscle cells. Hypertens Res, 1996, 19(1): 23-30.
[3]. Douglas SA, Gellai M, Ezekiel M, et al. BQ-123, a selective endothelin subtype A-receptor antagonist, lowers blood pressure in different rat models of hypertension. J Hypertens, 1994, 12(5): 561-567.
[4]. Büyükgebiz O, Aktan AO, Haklar G, et al. BQ-123, a specific endothelin (ETA) receptor antagonist, prevents ischemia-reperfusion injury in kidney transplantation. Transpl Int, 1996, 9(3): 201-207.
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