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156161-89-6

中文名稱 BQ-788 鈉鹽
英文名稱 BQ-788
CAS 156161-89-6
分子式 C34H50N5O7.Na
分子量 663.79
MOL 文件 156161-89-6.mol
更新日期 2024/11/15 18:20:29
156161-89-6 結(jié)構(gòu)式 156161-89-6 結(jié)構(gòu)式

基本信息

中文別名
BQ-788 鈉鹽
英文別名
CS-1494
BQ-788 SODIUM
BQ789 Sodium Salt
1-ELAIDYLPHOSPHOCHOLINE, >97%
BQ788 SODIUM SALT
BQ 788 SODIUM SALT
BQ-788 SYNTHETIC >97% ETB ENDOTHELIN REC EPT
N-[N-[N-[(2,6-Dimethyl-1-piperidinyl)carbonyl]-
N-cis-2,6-dimethylpiperidinocarbonyl-L-γMeLeu-D-Trp(COOMe)-D-Nle-ONa
2,6-Dimethylpiperidinecarbonyl-γ-Methyl-Leu-Nin-(Methoxycarbonyl)-D-Trp-D-Nle
DMpc-gaMMa-MeLeu-D-Trp(1-CO2CH3)-D-Nle.Na (DMpc : cis-2,6-DiMethylpiperidinocarbonyl)
所屬類別
生物:拮抗劑

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C
溶解度acetonitrile: 0.3 mg/mL
溶解度在乙腈中的溶解度:0.3 mg/mL
形態(tài)solid
顏色white

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
WGK Germany3
WGK Germany3

常見問題列表

生物活性
BQ-788 sodium salt 是一種有效,選擇性的 ETB 受體拮抗劑,在人類 Girrardi 心臟細(xì)胞中抑制 ET-1 與 ETB 受體結(jié)合的 IC50 為 1.2 nM。
靶點(diǎn)

IC50: 1.2 nM (ETB)

體外研究

BQ-788 potently and competitively inhibits 125 I-labeled ET-1 binding to ETB receptors in human Girrardi heart cells with an IC 50 of 1.2 nM, but only poorly inhibits the binding to ETA receptors in human neuro-blastoma cell line SK-N-MC cells (IC 50 , 1300 nM). BQ-788 shows no agonistic activity up to 10 μM and competitively inhibits thevasoconstriction induced by an ETB-selective agonist (pA2, 8.4). BQ-788 also inhibits several bioactivities of ET-1, such as bronchoconstriction, cell proliferation, and clearance of perfused ET-1.

體內(nèi)研究

BQ-788 (3 mg/kg/h, i.v.) completely inhibits a pharmacological dose of ET-1- or sarafotoxin6c (0.5 nmol/kg, i.v.)-induced ETB receptor-mediated depressor, but not pressor responses in conscious rats. Furthermore, BQ-788 markedly increases the plasma concentration of ET-1, which is considered an index of potential ETB receptor blockade in vivo. In Dahl salt-sensitive hypertensive (DS) rats, BQ-788 (3 mg/kg/h, i.v.) increases blood pressure by about 20 mm Hg. It is reported that BQ-788 also inhibits ET-1-induced bronchoconstriction, tumor growth and lipopolysaccharide-induced organfailure. BQ 788 (3 mg/kg) results in an eightfold leftward shift in the ET-1 dose-response curve, suggesting a significant involvement of ETB dilator receptors. Mice are treated with 30 nmol BQ-788 by intraplantar, reduce mechanical hyperalgesia (47% and 42%), thermal hyperalgesia (68% and 76%), oedema (50% and 30%); myeloperoxidase activity (64% and 32%), and overt-pain like behaviours. Additionally, intraplantar treatment with clazosentan or BQ-788 decreases spinal (45% and 41%) and peripheral (47% and 47%) superoxide anion production as well as spinal (47% and 47%) and peripheral (33% and 54%) lipid peroxidation, respectively.

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