BIBS 39

• Description :

  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. [1] 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.[1] 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. [2]

• UNSPSC :

  12352005

• Target :

  Angiotensin Receptor

• Type :

  Reference compound

• Related Pathways :

  GPCR/G Protein

• Applications :

  COVID-19-immunoregulation

• Field of Research :

  Cardiovascular Disease; Endocrinology

• Assay Protocol :

  https://www.medchemexpress.com/BIBS-39.html

• Concentration :

  10mM

• Purity :

  99.70

• Solubility :

  DMSO : ≥ 32 mg/mL

• Smiles :

  O=C(C1=CC=CC=C1C2=CC=C(CN3C4=CC(NC(NC5CCCCC5)=O)=CC=C4N=C3CCCC)C=C2)O

• Molecular Formula :

  C32H36N4O3

• Molecular Weight :

  524.65

• References & Citations :

  [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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  AT1 Receptor; AT2 Receptor

• CAS Number :

  [133085-33-3]