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Merck
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文件

B157

Sigma-Aldrich

BQ-788

≥95%, 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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About This Item

经验公式（希尔记法）:
C34H50N5NaO7
CAS号:
156161-89-6
分子量:
663.78
MDL號碼:
MFCD00797882
分類程式碼代碼:
12352200
PubChem物質ID:
329773192
NACRES:
NA.32

品質等級

200

化驗

≥95%

形狀

solid

顏色

white

溶解度

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

儲存溫度

−20°C

SMILES 字串

[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 密鑰

QCVIFBRTTLMEOV-FUKQNADPSA-M

基因資訊

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

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應用

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。

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

個人防護裝備

Eyeshields, Gloves, type N95 (US)

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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
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PloS one, 8(3), e58078-e58078 (2013-04-05)
Obstructive sleep apnoea (OSA) is a risk factor for cardiovascular disorders and in some cases is complication of pulmonary hypertension. We simulated OSA by exposing rats to cyclic intermittent hypoxia (CIH) to investigate its effect on pulmonary vascular endothelial dysfunction.
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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