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Documenti fondamentali

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B157

Sigma-Aldrich

BQ-788

≥95%, solid

Sinonimo/i:

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

Formula empirica (notazione di Hill):
C34H50N5NaO7
Numero CAS:
156161-89-6
Peso molecolare:
663.78
Numero MDL:
MFCD00797882
Codice UNSPSC:
12352200
ID PubChem:
329773192
NACRES:
NA.32

Livello qualitativo

200

Saggio

≥95%

Stato

solid

Colore

white

Solubilità

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

Temperatura di conservazione

−20°C

Stringa SMILE

[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
QCVIFBRTTLMEOV-FUKQNADPSA-M

Informazioni sul gene

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

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Applicazioni

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)

Azioni biochim/fisiol

Selective ETB endothelin receptor antagonist.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Dispositivi di protezione individuale

Eyeshields, Gloves, type N95 (US)

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Certificati d'analisi (COA)

Lot/Batch Number
SLCH9288
SLBZ1908
SLBS0689V
SLBM5550V
SLBK3267V

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Endothelin 1, Human and Porcine Endothelin 1, Human and Porcine, CAS 117399-94-7, is a 21-amino acid polypeptide with potent vasoconstrictive action. Activates phospholipase C in fibroblasts expressing ETA receptors.

Sigma-Aldrich

05-23-3800

Endothelin 1, Human and Porcine

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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