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Merck
CN

B157

Sigma-Aldrich

BQ-788

≥95%, endothelin-B (ETRB) blocker, solid

别名:

2,6-二甲基哌啶羰基-γ-甲基-亮氨酸-Nin-(甲氧羰基)-D-色氨酸-D-Nle, N-[N-[N-[(2,6-二甲基-1-哌啶基)羰基]-4-甲基-L-亮氨酰]-1-(甲氧基羰基)-D-色氨酰]-D-正亮氨酸 钠盐

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关于此项目

经验公式(希尔记法):
C34H50N5NaO7
CAS Number:
分子量:
663.78
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.32
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Product Name

BQ-788, ≥95%, solid

质量水平

方案

≥95%

表单

solid

颜色

white

溶解性

acetonitrile: 0.3 mg/mL
DMSO: 1.2 mg/mL
ethanol: 1.2 mg/mL
H2O: slightly soluble

储存温度

−20°C

SMILES字符串

[Na+].CCCC[C@@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@H](CC(C)(C)C)NC(=O)N3[C@@H](C)CCC[C@H]3C)C([O-])=O

InChI

1S/C34H51N5O7.Na/c1-8-9-16-25(31(42)43)35-29(40)26(18-23-20-38(33(45)46-7)28-17-11-10-15-24(23)28)36-30(41)27(19-34(4,5)6)37-32(44)39-21(2)13-12-14-22(39)3;/h10-11,15,17,20-22,25-27H,8-9,12-14,16,18-19H2,1-7H3,(H,35,40)(H,36,41)(H,37,44)(H,42,43);/q;+1/p-1/t21-,22+,25-,26-,27+;/m1./s1

InChI key

QCVIFBRTTLMEOV-FUKQNADPSA-M

基因信息

human ... EDNRB(1910)
mouse ... EDNRB(13618)
rat ... EDNRB(50672)

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应用

BQ-788 已被用作人气道平滑肌细胞 (HASMC)、子宫间皮细胞 (UtMC) 衍生的血管平滑肌细胞 (VSMC) 以及人脐静脉内皮细胞 (HUVEC) 的选择性内皮缩血管肽 (ETRB) 阻断剂。

生化/生理作用

选择性ETB内皮素受体拮抗剂。

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

Eyeshields, Gloves, type N95 (US)


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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PloS one, 7(10), e47662-e47662 (2012-10-19)
Two endothelin receptor antagonists (ERAs), bosentan and ambrisentan, are currently approved for the treatment of pulmonary arterial hypertension (PAH), a devastating disease involving an activated endothelin system and aberrant contraction and proliferation of pulmonary arterial smooth muscle cells (PASMC). The
Lenyta Oliveira Gomes et al.
The Journal of pharmacy and pharmacology, 70(7), 893-900 (2018-03-24)
This study assessed the ability of endothelin-1 (ET-1) to evoke heat hyperalgesia when injected directly into the trigeminal ganglia (TG) of mice and determined the receptors implicated in this effect. The effects of TG ETA and ETB receptor blockade on
Christophe Faisy et al.
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Lung inflation may have deleterious effects on the alveoli during mechanical ventilation. However, the consequences of stretch during excessive lung inflation on basal tone and responsiveness of human bronchi are unknown. This study was undertaken to devise an experimental model
H Karaki et al.
Biochemical and biophysical research communications, 205(1), 168-173 (1994-11-30)
The effects of a peptide, BQ-788 [N-cis-2, 6-dimethyl-piperidinocarbonyl-L-gamma-methylleucyl-D-1- methoxycarbonyltryptophanyl-D-norleucine], on isolated blood vessel and small intestine were examined. In the rat aorta, BQ-788 antagonized the endothelium-dependent, ETB1 receptor-mediated relaxation due to endothelin (ET)-3 with EC50 of 3 microM. In the

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