BQ-3020
目录号 : GC14416
A peptide ETB receptor antagonist
Cas No.:143113-45-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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 | |
| 化学名 | (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] | ||
| 分子式 | C96H140N20O25S | 分子量 | 2006.32 |
| 溶解度 | Soluble to 0.50 mg/ml in sodium bicarbonate (0.03M) | 储存条件 | Desiccate at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.4984 mL | 2.4921 mL | 4.9842 mL |
| 5 mM | 0.0997 mL | 0.4984 mL | 0.9968 mL |
| 10 mM | 0.0498 mL | 0.2492 mL | 0.4984 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。