>>Signaling Pathways>> GPCR/G protein>> Endothelin Receptor>>BQ-788 sodium salt

BQ-788 sodium salt

Catalog No.GC15916

BQ-788 나트륨염은 강력하고 선택적인 ETB 수용체 길항제로서 인간 Girradi 심장 세포에서 1.2 nM의 IC50으로 ETB 수용체에 대한 ET-1 결합을 억제합니다.

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BQ-788 sodium salt Chemical Structure

Cas No.: 156161-89-6

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$428.00
재고 있음
1mg
US$135.00
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5mg
US$293.00
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10mg
US$419.00
재고 있음

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Sample solution is provided at 25 µL, 10mM.

Description Protocol Chemical Properties Product Documents Related Products

BQ-788 is a potent and selective antagonist of endothelin (ET) B-receptor with IC50 value of 1.2nM [1].

In the in vitro assay, BQ-788 prevents ET-1 from binding to ETB receptors in human Girardi heart cells with IC50 value of 1.2nM. The inhibition to ETA receptors is much weaker with IC50 value of 1300nM. BQ-788 also inhibits ET binding to ETB receptors with IC50 values of 0.9nM and 1.2nM in porcine cerebellar membranes and hGH cells, respectively. The inhibition effects are quite poor in pCASM cells and SK-N-MC cells with IC50 values of 280nM and 1300nM, respectively. BQ-788 is specific to ET receptors. It cannot significantly inhibit other peptide hormone receptors at concentration of 10μM. It is found that BQ-788 interacts with ETB receptors competitively in hGH cells. Moreover, the in vivo assay demonstrates that ETB receptors are responsible for ET-1-elicited bronchoconstriction in guinea pigs [1].

References:
[1] Ishikawa K, Ihara M, Noguchi K, et al. Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proceedings of the National Academy of Sciences, 1994, 91(11): 4892-4896.

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