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BIBS 39

源叶(MedMol) 99%
  • 英文名:
  • BIBS 39
  • 别名:
  • Bibs 39
  • CAS号:
  • 133085-33-3
  • 分子式:
  • C31H34N4O3
  • 分子量:
  • 524.653
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源叶(MedMol) S82856-1mg 99% ¥580.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S82856-2mg 99% ¥1100.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S82856-5mg 99% ¥1900.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S82856-10mg 99% ¥3200.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S82856-25mg 99% ¥6400.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S82856-50mg 99% ¥8700.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: BIBS 39 is a new nonpeptide angiotensin II (AII) receptor antagonist. Target: Angiotensin Receptor in vitro: BIBS 39 displaces [125I] AII from its specific binding sites with a Ki value of 29 ± 7 nM for the AII subtype 1 (AT1) receptor and a Ki value of 480 ± 110 nM for the AII subtype 2 (AT2) receptor. BIBS 222 shows a Ki value of 20 ± 7 nM for the AT1 subtype and a Ki value of 730 ± 170 nM for the AT2 subtype. BIBS 39 is 17 times more selective for the AT1 subtype and BIBS 222 37 times. BIBS 39 shifts the AII concentration-contractile response curves in isolated rabbit aorta to the right in a parallel fashion. in vivo: In pithed rats, BIBS 39 dependently shifts the dose-response curve of AII to the right without affecting the maximal response. BIBS 222 also causes parallel shifts to the right but a significant reduction of the maximal responses was observed at 3 and 10 mg/kg i.v. These results show that the benzimidazole derivatives BIBS 39 is a potent and selective AII receptor antagonists. Substitution with a benzimidazole moiety results into a considerable loss of selectivity for the AT1 receptor subtype compared with an imidazole moiety as, for instance, in DuP 753.BIBS 39 is a new nonpeptide angiotensin receptor blockers that has affinity for both AT1- and AT2-receptors, is also a potent antagonist of the cardiovascular effects of AII in pithed rabbits.
  • 靶点: Angiotensin Receptor;RAAS
  • 参考文献:
    1. Zhang J, et al. Characterization of BIBS 39 and BIBS 222: two new nonpeptide angiotensin II receptor antagonists. Eur J Pharmacol. 1992 Jul 21;218(1):35-41. 2. Zhang J, et al. Hemodynamic effects of angiotensin II and the influence of angiotensin receptor antagonists in pithed rabbits. J Cardiovasc Pharmacol. 1995 May;25(5):724-31.
  • 溶解性: Soluble  in  DMSO
  • 保存条件: 2-8℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.906 ml 9.53 ml 19.06 ml
    5 mM 0.381 ml 1.906 ml 3.812 ml
    10 mM 0.191 ml 0.953 ml 1.906 ml
    50 mM 0.038 ml 0.191 ml 0.381 ml
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