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Merck
모든 사진(1)

주요 문서

B157

Sigma-Aldrich

BQ-788

≥95%, solid

동의어(들):

2,6-Dimethylpiperidinecarbonyl-γ-Methyl-Leu-Nin-(Methoxycarbonyl)-D-Trp-D-Nle, N-[N-[N-[(2,6-Dimethyl-1-piperidinyl)carbonyl]-4-methyl-L-leucyl]-1-(methoxycarbonyl)-D-tryptophyl]-D-norleucine sodium salt

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About This Item

실험식(Hill 표기법):
C34H50N5NaO7
CAS Number:
Molecular Weight:
663.78
MDL number:
UNSPSC 코드:
12352200
PubChem Substance ID:
NACRES:
NA.32

Quality Level

분석

≥95%

양식

solid

색상

white

solubility

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

저장 온도

−20°C

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

유전자 정보

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

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애플리케이션

BQ-788 has been used as a selective endothelin-B (ETRB) blocker in human airway smooth muscle cells (HASMCs), uterine mesothelial cells (UtMCs)-derived vascular smooth muscle cells (VSMCs), and human umbilical vein endothelial cells (HUVECs)

생화학적/생리학적 작용

Selective ETB endothelin receptor antagonist.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

개인 보호 장비

Eyeshields, Gloves, type N95 (US)


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문서 라이브러리 방문

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
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
John Gatfield et al.
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
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
Zhuo Wang et al.
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.

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