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Merck
CN

B157

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
化学文摘社编号:
156161-89-6
分子量:
663.78
UNSPSC Code:
12352200
PubChem Substance ID:
329773192
NACRES:
NA.32
MDL number:
MFCD00797882

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产品名称

BQ-788, ≥95%, solid

SMILES string

[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

assay

≥95%

form

solid

color

white

solubility

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

storage temp.

−20°C

Quality Level

200

Gene Information

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

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相关类别

Application

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。

Biochem/physiol Actions

选择性ETB内皮素受体拮抗剂。

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000519739
0000519739
0000496221
0000496221
0000488460

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Emilia Kansanen et al.
Molecular pharmacology, 92(4), 481-490 (2017-08-06)
Nitro-fatty acids are reactive signaling mediators that are formed when unsaturated fatty acids react with nitric oxide or nitric oxide-derived species. Nitro-fatty acids can modify specific signaling pathways via post-translational modifications of Cys residues in key regulatory proteins. One of
Emilie Hitzerd et al.
Hypertension (Dallas, Tex. : 1979), 75(3), 877-884 (2019-12-31)
Increasing evidence suggests a role for the ET (endothelin) system in preeclampsia. Hence, blocking this system with endothelin receptor antagonists (ERAs) could be a therapeutic strategy. Yet, clinical studies are lacking due to possible teratogenic effects of ERAs. In this
Takeshi Nakahara et al.
Scientific reports, 10(1), 9510-9510 (2020-06-13)
Endothelin-1 (ET-1) is well known as the most potent vasoconstrictor, and can evoke histamine-independent pruritus. Recently, its involvement in cutaneous inflammation has begun to draw attention. The upregulation of ET-1 expression in the epidermis of human psoriasis patients has been
Christian Claude Lachaud et al.
PloS one, 8(2), e55181-e55181 (2013-02-14)
In mammalian visceral organs, vascular smooth muscle cells (VSMCs) originate from an epithelial-to-mesenchymal transition (EMT) of embryonic mesothelial cells (MCs). The ability of adult MCs to recapitulate EMT and to acquire smooth muscle (SM) markers upon provasculogenic culture suggested they
Ovidiu Constantin Baltatu et al.
Frontiers in physiology, 3, 103-103 (2012-04-25)
Several clinical studies have investigated the potential benefits of endothelin receptor antagonism in chronic pathologies such as diabetic kidney disease. However, fluid retention and edema have been identified as major side effects of endothelin receptor antagonists. In the present study
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