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| | BIBS 39 Basic information |
| Product Name: | BIBS 39 | | Synonyms: | BIBS 39;CS-2534;BIBS 39; BIBS-39;2-[4-[[2-butyl-6-(cyclohexylcarbamoylamino)benzimidazol-1-yl]methyl]phenyl]benzoic acid;[1,1'-Biphenyl]-2-carboxylic acid, 4'-[[2-butyl-6-[[(cyclohexylamino)carbonyl]amino]-1H-benzimidazol-1-yl]methyl]-;4'-({2-butyl-6-[(cyclohexylcarbamoyl)amino]-1H-1,3-benzodiazol-1-yl}methyl)-[1,1'-biphenyl]-2-carboxylic acid;4'-((2-butyl-6-(3-cyclohexylureido)-1H-benzo[d]imidazol-1-yl)methyl)-[1,1'-biphenyl]-2-carboxylic acid | | CAS: | 133085-33-3 | | MF: | C32H36N4O3 | | MW: | 524.65 | | EINECS: | | | Product Categories: | | | Mol File: | 133085-33-3.mol |  |
| | BIBS 39 Chemical Properties |
| Boiling point | 729.1±60.0 °C(Predicted) | | density | 1.24±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMF:30.0(Max Conc. mg/mL);57.18(Max Conc. mM)
DMSO:30.0(Max Conc. mg/mL);57.18(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.48(Max Conc. mM) | | form | A crystalline solid | | pka | 3.84±0.36(Predicted) | | color | White to off-white |
| | BIBS 39 Usage And Synthesis |
| Uses | 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] | | IC 50 | AT2 Receptor; AT1 Receptor | | References | [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. DOI:10.1016/0014-2999(92)90144-s
[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. DOI:10.1097/00005344-199505000-00007 |
| | BIBS 39 Preparation Products And Raw materials |
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