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Datasheet of BQ-788

Description:.
BQ-788 sodium salt is a potent, selective ETB receptor antagonist (IC50 = 1.2 nM for inhibition of ET-1 binding to human
Girardi heart cells); poorly inhibited the binding to ET A receptors in human neuroblastoma cell line SK-N-MC cells (IC(50),
1300 nM).
in vitro: BQ-788 potently and competitively inhibited (125)I-labeled ET-1 binding to ET(B) receptors in human Girrardi heart
cells (hGH) with an IC(50) of 1.2 nM, but only poorly inhibited the binding to ET A receptors in human neuroblastoma cell line
SK-N-MC cells (IC(50), 1300 nM). In isolated rabbit pulmonary arteries, BQ-788 showed no agonistic activity up to 10 microM
and competitively inhibited the vasoconstriction induced by an ET(B)-selective agonist (pA(2), 8.4). BQ-788 also inhibited
several bioactivities of ET-1, such as bronchoconstriction, cell proliferation, and clearance of perfused ET-1 [1]. 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 rat aorta without endothelium, 10 microM BQ-788 weakly antagonized the ETA1-mediated contractile effects of
ET-1 and ET-3.
in vivo: In conscious rats, BQ-788, 3 mg/kg/h, i.v., completely inhibited a pharmacological dose of ET-1- or sarafotoxin6c (S6c)
(0.5 nmol/kg, i.v.)-induced ET(B) receptor-mediated depressor, but not pressor responses. Furthermore, BQ-788 markedly
increased the plasma concentration of ET-1, which is considered an index of potential ET(B) receptor blockade in vivo. In Dahl
salt-sensitive hypertensive (DS) rats, BQ-788, 3 mg/kg/h, i.v., increased blood pressure by about 20 mm Hg. It is reported that
BQ-788 also inhibited ET-1-induced bronchoconstriction, tumor growth and lipopolysaccharide-induced organ failure. BQ 788
(3 mg/kg) resulted in an eightfold leftward shift in the ET-1 dose-response curve, suggesting a significant involvement of ETB
dilator receptors. In the absence or presence of BQ 788, each ET antagonist evoked a rightward shift from vehicle. With the
exception of BMS 182874, BQ 788 increased the magnitude of the shifts

Chemical Information
Catalog

DC7542

Purity of current batch:

>98%

Molecular Weight (MW)

663.78

Molecular Formula

C34H50N5NaO7

CAS No.

156161-89-6

Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.