BQ-788 sodium salt
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
BQ-788是一种有效的内皮缩(ET)B受体选择性拮抗剂,IC50值为1.2 nM[1].
在体外试验中,BQ-788阻止人Girardi心脏细胞中ET-1与ETB受体结合,IC50值为1.2 nM.对ETA受体的抑制作用更弱,IC50值为1300 nM. BQ-788也抑制猪小脑膜和 hGH细胞中ET与ETB受体的结合,IC50值分别为0.9 nM和1.2 nM.对pCASM细胞和SK-N-MC细胞的抑制作用相当弱,IC50值分别为280 nM和1300 nM.BQ-788对ET受体具有特异性.在浓度为10 μM时,不能显著抑制其他肽类激素受体.在hGH细胞中,BQ-788与ETB受体竞争性相互作用.此外,豚鼠体内实验表明,ETB受体与ET-1诱发的支气管狭窄有关[1].
参考文献:
[1] Ishikawa K, Ihara M, Noguchi K, et al. Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proceedings of the National Academy of Sciences, 1994, 91(11): 4892-4896.
- 1. Juliano T. Freitas, Jesus Lopez, et al. "The immunosuppressive role of Edn3 over‐expression in the melanoma microenvironment." Pigment Cell Melanoma Res. 2021 Nov;34(6):1084-1093. PMID:34288510
- 2. Huang X, Chen C, et al. "Transdermal BQ-788/EA@ZnO quantum dots as targeting and smart tyrosinase inhibitors in melanocytes." Mater Sci Eng C Mater Biol Appl. 2019 Sep;102:45-52. PMID:31147016
Physical Appearance | A solid |
Storage | Desiccate at RT |
M.Wt | 663.78 |
Cas No. | 156161-89-6 |
Formula | C34H50N5NaO7 |
Solubility | ≥33.2 mg/mL in DMSO; ≥2.71 mg/mL in H2O with gentle warming and ultrasonic; ≥16.2 mg/mL in EtOH |
Chemical Name | sodium;(2R)-2-[[(2R)-2-amino-3-(1-methoxycarbonylindol-3-yl)propanoyl]-[(2S)-2-[[(2R,6S)-2,6-dimethylpiperidine-1-carbonyl]amino]-4,4-dimethylpentanoyl]amino]hexanoate |
SDF | Download SDF |
Canonical SMILES | CCCCC(C(=O)[O-])N(C(=O)C(CC1=CN(C2=CC=CC=C21)C(=O)OC)N)C(=O)C(CC(C)(C)C)NC(=O)N3C(CCCC3C)C.[Na+] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
hGH和pCASM细胞 |
制备方法 |
在DMSO中的溶解度大于33.2 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
100 μM |
实验结果 |
BQ-788 (100 μM) 不增加hGH和pCASM细胞中的[Ca2+]i。然而,在上述2种细胞系中,BQ-788显著抑制ET-1诱导的[Ca2+]i增加。 |
动物实验 [1]: | |
动物模型 |
大鼠 |
给药剂量 |
1 mg/kg;静脉注射 |
实验结果 |
在注射ET-1 5分钟前,静脉注射1 mg/kg BQ-788完全抑制降压作用,相应地引起快速而明显的增压作用。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1]. Ishikawa K, Ihara M, Noguchi K, et al. Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proceedings of the National Academy of Sciences, 1994, 91(11): 4892-4896. |
质量控制和MSDS
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