Product Name :
BIBS 39
Description:
BIBS 39 is a new nonpeptide angiotensin II (AII) receptor antagonist.Target: Angiotensin Receptorin 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.
CAS:
133085-33-3
Molecular Weight:
524.65
Formula:
C32H36N4O3
Chemical Name:
4′-({2-butyl-6-[(cyclohexylcarbamoyl)amino]-1H-1,3-benzodiazol-1-yl}methyl)-[1,1′-biphenyl]-2-carboxylic acid
Smiles :
CCCCC1=NC2=CC=C(C=C2N1CC1C=CC(=CC=1)C1=CC=CC=C1C(O)=O)NC(=O)NC1CCCCC1
InChiKey:
OLQFKFSAJNUOPT-UHFFFAOYSA-N
InChi :
InChI=1S/C32H36N4O3/c1-2-3-13-30-35-28-19-18-25(34-32(39)33-24-9-5-4-6-10-24)20-29(28)36(30)21-22-14-16-23(17-15-22)26-11-7-8-12-27(26)31(37)38/h7-8,11-12,14-20,24H,2-6,9-10,13,21H2,1H3,(H,37,38)(H2,33,34,39)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Anti-Mouse IL-10 Antibody} web|{Anti-Mouse IL-10 Antibody} Interleukin Related|{Anti-Mouse IL-10 Antibody} Technical Information|{Anti-Mouse IL-10 Antibody} References|{Anti-Mouse IL-10 Antibody} custom synthesis|{Anti-Mouse IL-10 Antibody} Epigenetics}
Shelf Life:
≥12 months if stored properly.{{Affinity Chromatography Column} MedChemExpress|{Affinity Chromatography Column} NF-κB|{Affinity Chromatography Column} Protocol|{Affinity Chromatography Column} References|{Affinity Chromatography Column} supplier}
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
BIBS 39 is a new nonpeptide angiotensin II (AII) receptor antagonist.Target: Angiotensin Receptorin 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.PMID:27217159 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.|Product information|CAS Number: 133085-33-3|Molecular Weight: 524.65|Formula: C32H36N4O3|Chemical Name: 4′-({2-butyl-6-[(cyclohexylcarbamoyl)amino]-1H-1,3-benzodiazol-1-yl}methyl)-[1,1′-biphenyl]-2-carboxylic acid|Smiles: CCCCC1=NC2=CC=C(C=C2N1CC1C=CC(=CC=1)C1=CC=CC=C1C(O)=O)NC(=O)NC1CCCCC1|InChiKey: OLQFKFSAJNUOPT-UHFFFAOYSA-N|InChi: InChI=1S/C32H36N4O3/c1-2-3-13-30-35-28-19-18-25(34-32(39)33-24-9-5-4-6-10-24)20-29(28)36(30)21-22-14-16-23(17-15-22)26-11-7-8-12-27(26)31(37)38/h7-8,11-12,14-20,24H,2-6,9-10,13,21H2,1H3,(H,37,38)(H2,33,34,39)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : ≥ 32 mg/mL (60.99 mM).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|Products are for research use only. Not for human use.|