| Identification | Back Directory | [Name]
BIBS 39 | [CAS]
133085-33-3 | [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]- | [Molecular Formula]
C32H36N4O3 | [MOL File]
133085-33-3.mol | [Molecular Weight]
524.65 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 | [storage]
Store at -20°C | [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 |
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D&C Chemicals
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