BQ-788
目录号 : GC35546
A peptide ETB receptor antagonist
Cas No.:173326-37-9
Sample solution is provided at 25 µL, 10mM.
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BQ-788 is a peptide endothelin type B (ETB) receptor antagonist (IC50 = 1.2 nM).1 It is selective for ETB over ETA receptors (IC50 = 280 nM), as well as angiotensin, calcitonin, or neuropeptide receptors at 10 ?M. BQ-788 inhibits calcium mobilization induced by endothelin-1 (ET-1) in human Girrardi heart cells (IC50 = 0.54 nM) and vasoconstriction induced by the ETB-selective agonist BQ-3020 in isolated rat pulmonary arteries (pA2 = 8.4).2 In vivo, BQ-788 (1 mg/kg, i.v.) inhibits ET-1-induced depressor responses and induces pressor responses in rats. It protects against laparotomy and surgical gut handling-induced inhibition of intestinal motility in rats.3 BQ-788 also attenuates delayed hypotension, vascular hyporeactivity to norepinephrine, and hepatocellular injury and dysfunction in a rat model of LPS-induced endotoxemia.4
1.Okada, M., and Nishikibe, M.BQ-788, a selective endothelin ETB receptor antagonistCardiovasc. Drug Rev.20(1)53-66(2002) 2.Ishikawa, K., Ihara, M., Noguchi, K., et al.Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788Proc. Natl. Acad. Sci. USA91(11)4892-4896(1994) 3.?ugowska-Umer, H., Umer, A., Kuziemski, K., et al.The protective effect of endothelin receptor antagonists against surgically induced impairment of gastrointestinal motility in ratsJ. Smooth Muscle Res.5523-33(2019) 4.Ruetten, H., and Thiemermann, C.Effect of selective blockade of endothelin ETB receptors on the liver dysfunction and injury caused by endotoxaemia in the ratBr. J. Pharmacol.119(3)479-486(1996)
| Cas No. | 173326-37-9 | SDF | |
| Canonical SMILES | CCCC[C@H](C(O)=O)NC([C@@H](CC1=CN(C(OC)=O)C2=CC=CC=C12)NC([C@H](CC(C)(C)C)NC(N3[C@H](C)CCC[C@@H]3C)=O)=O)=O | ||
| 分子式 | C34H51N5O7 | 分子量 | 641.8 |
| 溶解度 | DMSO : 100 mg/mL (155.81 mM; Need ultrasonic) | 储存条件 | Store at -20°C,protect from light |
| 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 | 1.5581 mL | 7.7906 mL | 15.5812 mL |
| 5 mM | 0.3116 mL | 1.5581 mL | 3.1162 mL |
| 10 mM | 0.1558 mL | 0.7791 mL | 1.5581 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet