BQ-788 钠盐 CAS#: 156161-89-6

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BQ-788 钠盐

生物活性靶点体外研究体内研究

中文名称	BQ-788 钠盐
中文同义词	BQ-788 钠盐;化合物 T10595L;(R)-2-((R)-2-((S)-2-((2R,6S)-2,6-二甲基哌啶-1-甲酰胺基)-4,4-二甲基戊酰胺)-3-(1-(甲氧基羰基)-1H-吲哚-3-基)丙酰胺基)己酸钠盐;化合物 BQ-788 SODIUM SALT
英文名称	BQ-788
英文同义词	BQ-788 SODIUM;BQ-788 SYNTHETIC >97% ETB ENDOTHELIN REC EPT;N-[(cis-2,6-Dimethyl-1-piperidinyl)carbonyl]-4-methyl-L-leucyl-1-(methoxycarbonyl)-D-tryptophyl-D-norleucinesodiumsalt;1-ELAIDYLPHOSPHOCHOLINE, >97%;N-[N-[N-[(2,6-Dimethyl-1-piperidinyl)carbonyl]-4-methyl-L-leucyl]-1-(methoxycarbonyl)-D-tryptophyl]-D-norleucine  sodium  salt,  2,6-Dimethylpiperidinecarbonyl-γ-Methyl-Leu-Nin-(Methoxycarbonyl)-D-Trp-D-Nle;N-[N-[N-[(2,6-Dimethyl-1-piperidinyl)carbonyl]-;DMpc-gaMMa-MeLeu-D-Trp(1-CO2CH3)-D-Nle.Na (DMpc : cis-2,6-DiMethylpiperidinocarbonyl);2,6-Dimethylpiperidinecarbonyl-γ-Methyl-Leu-Nin-(Methoxycarbonyl)-D-Trp-D-Nle
CAS号	156161-89-6
分子式	C34H52N5NaO7
分子量	665.81
EINECS号
相关类别	Endothelin receptor
Mol文件	156161-89-6.mol
结构式

BQ-788 钠盐 性质

BQ-788 钠盐 用途与合成方法

生物活性

BQ-788 sodium salt 是一种有效，选择性的 ETB  受体拮抗剂，在人类 Girrardi 心脏细胞中抑制 ET-1 与 ETB 受体结合的 IC50 为 1.2 nM。

靶点

IC50: 1.2 nM (ETB)

体外研究

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.

体内研究

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.

安全信息

MSDS信息

BQ-788 钠盐 上下游产品信息