BQ-123
(Synonyms: 环(D-ALPHA-天冬氨酰-L-脯氨酰-D-缬氨酰-L-亮氨酰-D-色氨酰)) 目录号 : GC15887
A peptide ETA receptor antagonist
Cas No.:136553-81-6
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-123 is a potent and selective antagonist of ETA endothelin receptor with Ki values of 1.4 and 1500 nM for ETA and ETB receptors, respectively.
Endothelin receptor is a G protein-coupled receptor. ETA receptor increases intracellular-free Ca2+. Also, Activation of ETA receptor increases vasoconstriction and blood pressure.
BQ-123 is a selective ETA receptor antagonist. In the ETA-expressing cells, BQ123 (10-6 M) inhibited endothelin-1 (ET-1) (10-6 M)-induced [Ca2+]i increase by 95% [1]. In rat vascular smooth muscle cells (VSMC), BQ-123 inhibited ET-1 receptor binding, cellular contraction, [Ca2+ ]i mobilization, [3H]thymidine incorporation, MAP kinase activation and MTT reduction induced by ET-1. However, BQ-123 didn’t inhibit angiotensin II (Ang II)- and arginine vasopressin (AVP)-induced increases in MAP kinase activity and [Ca2+]i mobilization [2].
In spontaneously hypertensive rats (SHR), renin hypertensive rats and normotensive rats, BQ-123 (16 nM/kg/min) reduced mean arterial pressure in a dose-dependent way in SHR. Also, BQ-123 lowered blood pressure in both renin hypertensive rats and normotensive rats [3]. In a kidney transplantation rat model with reperfusion injury, BQ-123 prevented reperfusion injury and inhibited the synthesis and release of ET-1,2 [4].
References:
[1]. Sakamoto A, Yanagisawa M, Sawamura T, et al. Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonist and endothelinB-selective agonists. J Biol Chem, 1993, 268(12): 8547-8553.
[2]. Guo X, Okada K, Fujita N, et al. Inhibitory effect of BQ-123 on endothelin-1-stimulated mitogen-activated protein kinase and cell growth of rat vascular smooth muscle cells. Hypertens Res, 1996, 19(1): 23-30.
[3]. Douglas SA, Gellai M, Ezekiel M, et al. BQ-123, a selective endothelin subtype A-receptor antagonist, lowers blood pressure in different rat models of hypertension. J Hypertens, 1994, 12(5): 561-567.
[4]. Büyükgebiz O, Aktan AO, Haklar G, et al. BQ-123, a specific endothelin (ETA) receptor antagonist, prevents ischemia-reperfusion injury in kidney transplantation. Transpl Int, 1996, 9(3): 201-207.
| Cas No. | 136553-81-6 | SDF | |
| 别名 | 环(D-ALPHA-天冬氨酰-L-脯氨酰-D-缬氨酰-L-亮氨酰-D-色氨酰) | ||
| 化学名 | 2-((3R,6S,9S,12S,17aS)-9-((1H-indol-3-yl)methyl)-6-isobutyl-3-isopropyl-1,4,7,10,13-pentaoxohexadecahydro-1H-pyrrolo[1,2-a][1,4,7,10,13]pentaazacyclopentadecin-12-yl)acetic acid | ||
| Canonical SMILES | O=C([C@H]1N(C([C@H](CC(O)=O)NC([C@H](CC2=CNC3=CC=CC=C23)NC4=O)=O)=O)CCC1)N[C@@H](C(N[C@H]4CC(C)C)=O)C(C)C | ||
| 分子式 | C31H42N6O7 | 分子量 | 611 |
| 溶解度 | DMF: 1 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml,PBS (pH 7.2): slightly | 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 | 1.6367 mL | 8.1833 mL | 16.3666 mL |
| 5 mM | 0.3273 mL | 1.6367 mL | 3.2733 mL |
| 10 mM | 0.1637 mL | 0.8183 mL | 1.6367 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。