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B150

BQ-123

Name: BQ-123
Brand: SIGMA

≥99%, sodium salt, lyophilized powder

Synonym(s):

BQ123, Cyclo(D-Trp-D-Asp-Pro-D-Val-Leu)

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About This Item

Empirical Formula (Hill Notation):

C₃₁H₄₁N₆O₇Na

CAS Number:

136553-81-6

Molecular Weight:

632.68

NACRES:

NA.32

PubChem Substance ID:

24891595

UNSPSC Code:

12352204

MDL number:

MFCD00133204

Assay:

≥99%

Form:

lyophilized powder

Quality level:

200

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Quality Level

200

assay

≥99%

form

lyophilized powder

storage temp.

−20°C

SMILES string

[H][C@@]12CCCN1C(=O)[C@@H](CC(O)=O)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC2=O)C(C)C

InChI

1S/C31H42N6O7/c1-16(2)12-21-27(40)33-22(13-18-15-32-20-9-6-5-8-19(18)20)28(41)35-23(14-25(38)39)31(44)37-11-7-10-24(37)29(42)36-26(17(3)4)30(43)34-21/h5-6,8-9,15-17,21-24,26,32H,7,10-14H2,1-4H3,(H,33,40)(H,34,43)(H,35,41)(H,36,42)(H,38,39)/t21-,22+,23+,24-,26+/m0/s1

InChI key

VYCMAAOURFJIHD-PJNXIOHISA-N

Gene Information

human ... EDNRA(1909), EDNRB(1910)
rat ... Ednra(24326), Ednrb(50672)

Application

BQ-123 has been used as a selective endothelin-A receptor antagonist to study its effects on tumor necrosis factor α (TNFα)-induced human airway smooth muscle cells (HASMCs) proliferation. It is also used as endothelin-A receptor antagonist to study its effects on TNFα-induced granulocyte–macrophage colony-stimulating factor (GM-CSF) expression.

Biochem/physiol Actions

BQ-123 is an endothelin(Et) receptor antagonist and is exquisite for endothelin A (ETA) receptor. It is a cyclic pentapeptide.

Selective ET_A endothelin receptor antagonist.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

Regulatory Information

常规特殊物品

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Certificates of Analysis (COA)

Lot/Batch Number

0000484169

0000411543

0000253737

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TNFalpha-induced GM-CSF release from human airway smooth muscle cells depends on activation of an ET-1 autoregulatory positive feedback mechanism.

J Knobloch et al.

Thorax, 64(12), 1044-1052 (2009-10-24)

There is an urgent need to inhibit endothelin-1 (ET-1) induced chronic inflammatory processes in early stages of lung diseases in order to prevent untreatable irreversible stages often accompanied by lung fibrosis and pulmonary hypertension. Nothing is known about the airway

BQ-123, a peptidic endothelin ETA receptor antagonist, prevents the early cerebral vasospasm following subarachnoid hemorrhage after intracisternal but not intravenous injection.

M Clozel et al.

Life sciences, 52(9), 825-834 (1993-01-01)

The aim of this study was to evaluate the role of endothelin and endothelin ETA receptor in the early cerebral vasoconstriction following subarachnoid hemorrhage (SAH) in the rat. SAH induced by injection of autologous blood in the cisterna magna reduced

Effect of endothelinA-receptor antagonist BQ-123 and phosphoramidon on cerebral vasospasm.

F Cosentino et al.

Journal of cardiovascular pharmacology, 22 Suppl 8, S332-S335 (1993-01-01)

The present study was designed to determine whether an endothelinA (ETA)-receptor antagonist BQ-123 (cyclo[Dtrp, Dasp, pro-D-Val-Leu]) or an ET-converting enzyme inhibitor phosphoramidon may prevent development of cerebral vasospasm after subarachnoid hemorrhage (SAH). A "double hemorrhage" canine model of the disease

Reversal of established responses to endothelin-1 in vivo and in vitro by the endothelin receptor antagonists, BQ-123 and PD 145065.

T D Warner et al.

British journal of pharmacology, 112(1), 207-213 (1994-05-01)

1. Endothelin-1 binds almost irreversibly to its receptors and causes prolonged vasoconstrictions. Here we have studied the reversal of established responses to ET-1 in vivo and in vitro by BQ-123, an ETA receptor-selective antagonist, and/or PD 145065, an ETA/ETB receptor

Mouse connective tissue mast cell proteases tryptase and carboxypeptidase A3 play protective roles in itch induced by endothelin-1.

Elín I Magnúsdóttir et al.

Journal of neuroinflammation, 17(1), 123-123 (2020-04-24)

Itch is an unpleasant sensation that can be debilitating, especially if it is chronic and of non-histaminergic origin, as treatment options are limited. Endothelin-1 (ET-1) is a potent endogenous vasoconstrictor that also has the ability to induce a burning, non-histaminergic

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Global Trade Item Number

SKU	GTIN
B150-1MG	04061835435746
B150-200UG	04061833426128

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