BIBS 39 |
| Katalog-Nr.GC19071 |
BIBS 39 ist ein neuer nicht-peptidischer Angiotensin II (AII)-Rezeptorantagonist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 133085-33-3
Sample solution is provided at 25 µL, 10mM.
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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. [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]
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.
[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.
| Cas No. | 133085-33-3 | SDF | |
| Canonical SMILES | O=C(C1=CC=CC=C1C2=CC=C(CN3C4=CC(NC(NC5CCCCC5)=O)=CC=C4N=C3CCCC)C=C2)O | ||
| Formula | C32H36N4O3 | M.Wt | 524.65 |
| Löslichkeit | DMSO : ≥ 32 mg/mL (60.99 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.906 mL | 9.5302 mL | 19.0603 mL |
| 5 mM | 0.3812 mL | 1.906 mL | 3.8121 mL |
| 10 mM | 0.1906 mL | 0.953 mL | 1.906 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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