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Merck

B157

Sigma-Aldrich

BQ-788

≥95%, solid

Sinónimos:

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

Fórmula empírica (notación de Hill):
C34H50N5NaO7
Número de CAS:
Peso molecular:
663.78
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.32

Quality Level

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

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

Gene Information

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

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Application

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)

Biochem/physiol Actions

Selective ETB endothelin receptor antagonist.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)


Certificados de análisis (COA)

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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
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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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