BQ-3020 |
カタログ番号GC14416
One-Click Copy Product Info
|
ETB受容体アゴニスト、強力かつ選択的
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 143113-45-5
Sample solution is provided at 25 µL, 10mM.
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BQ-3020 is a linear endothelin (ET) analog that is highly selective for ETB receptors. It displaces [125I] ET-1 binding to ETB receptors in porcine cerebellar membranes with an IC50 value of 0.2 nM [1].
ET-1, a 21-amino acid peptide, is one of known isoforms of endothelin (ET-1, ET-2, ET-3), it has strong vasoconstrictor and mitogenic activity. ETB receptor is one of endothelin receptors (i.e. ETA and ETB). ETB receptor has nearly the same affinity for all endothelin isoforms [2].
BQ-3020 displaced [125I] ET-1 binding to ETB receptors in porcine cerebellar membranes at a concentration 4,700 times lower than that to ETA receptors (selective to ET-1) on aortic vascular smooth muscle cells (IC50: 940 nM) [1].
In eight healthy men aged from 20-28 years, the local response of Sarafotoxin S6c (SFTX6c) (5 pmol/min) or BQ-3020 (50 pmol/min) to intra-arterial or intravenous infusion was assessed. Comparing these studies, there was no significant difference between baseline measurements. All the effects were just in the infused arm. Following intra-arterial infusion, both SFTX6c and BQ-3020 produced vasoconstriction indicated by the reduction in forearm blood flow (-25±7% and -27±7%, respectively). Following intravenous infusion, both SFTX6c and BQ-3020 produced a vein diameter reduction (-30±8% and -16±7%, respectively) [3].
References:
[1]. Ihara M, Saeki T, Fukuroda T, et al. A novel radioligand [125I]BQ-3020 selective for endothelin (ETB) receptors. Life Sci., 1992, 51(6):PL47-52.
[2]. Seo B, Oemar BS, Siebenmann R, et al. Both ETA and ETB receptors mediate contraction to endothelin-1 in human blood vessels. Circulation, 1994, 89(3):1203-8.
[3]. Strachan FE, Crockett TR, Mills NL, et al. Constriction to ETB receptor agonists, BQ-3020 and sarafotoxin S6c, in human resistance and capacitance vessels in vivo. Br J Clin Pharmacol., 2000, 50(1):27-30.
| Cas No. | 143113-45-5 | SDF | |
| Chemical Name | (2S,3Z,5S,6Z,8S,9Z,11S,12Z,14S,15Z,17S,18Z,20S,21Z,23S,24Z,26S,27Z,29S,30Z,32S,33Z,35S,36Z,38S,39Z,41S)-17-((1H-imidazol-5-yl)methyl)-2-((1H-indol-3-yl)methyl)-38-(4-aminobutyl)-23-benzyl-5,8-di((S)-sec-butyl)-35-(2-carboxyethyl)-11-(carboxymethyl)-4,7,10 | ||
| Canonical SMILES | CC[C@]([C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/C)([H])CC(C)C)([H])CCSC)([H])CC(O)=O)([H])CCCCN)([H] | ||
| Formula | C96H140N20O25S | M.Wt | 2006.32 |
| 溶解度 | Soluble to 0.50 mg/ml in sodium bicarbonate (0.03M) | Storage | Desiccate 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 | 498.4 μL | 2.4921 mL | 4.9842 mL |
| 5 mM | 99.7 μL | 498.4 μL | 996.8 μL |
| 10 mM | 49.8 μL | 249.2 μL | 498.4 μL |
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μL
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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 saline, 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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)