BQ-788 钠盐
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- CAS号:
- 156161-89-6
- 英文名:
- BQ-788
- 英文别名:
- 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)
- 中文名:
- BQ-788 钠盐
- 中文别名:
- BQ-788 钠盐;化合物 T10595L
- CBNumber:
- CB7710904
- 分子式:
- C34H52N5NaO7
- 分子量:
- 665.81
- MOL File:
- 156161-89-6.mol
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BQ-788 钠盐化学性质
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储存条件:
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-20°C
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溶解度:
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acetonitrile: 0.3 mg/mL
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形态:
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solid
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颜色:
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white
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BQ-788 钠盐性质、用途与生产工艺
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。
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.
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.
BQ-788 钠盐
上下游产品信息
上游原料
下游产品
156161-89-6, BQ-788 钠盐 相关搜索:
- Endothelin receptor
- C34H51N5NaO7
- C34H50N5NaO7
- C34H50N5O7Na
- 化合物 T10595L
- BQ-788 钠盐
- 156161-89-6
- D-Norleucine, N-[[(2R,6S)-2,6-dimethyl-1-piperidinyl]carbonyl]-4-methyl-L-leucyl-1-(methoxycarbonyl)-D-tryptophyl-, sodium salt (1:1)
- sodium,(2R)-2-[[(2R)-2-amino-3-(1-methoxycarbonylindol-3-yl)propanoyl]-[(2S)-2-[[(2R,6S)-2,6-dimethylpiperidine-1-carbonyl]amino]-4,4-dimethylpentanoyl]amino]hexanoate
- CS-1494
- BQ788 SODIUM SALT; BQ 788 SODIUM SALT
- N-cis-2,6-dimethylpiperidinocarbonyl-L-γMeLeu-D-Trp(COOMe)-D-Nle-ONa
- BQ789 Sodium Salt
- 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
- DMpc-gaMMa-MeLeu-D-Trp(1-CO2CH3)-D-Nle.Na (DMpc : cis-2,6-DiMethylpiperidinocarbonyl)
- N-[N-[N-[(2,6-Dimethyl-1-piperidinyl)carbonyl]-
- 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
- 1-ELAIDYLPHOSPHOCHOLINE, >97%
- N-[(cis-2,6-Dimethyl-1-piperidinyl)carbonyl]-4-methyl-L-leucyl-1-(methoxycarbonyl)-D-tryptophyl-D-norleucinesodiumsalt
- BQ-788 SYNTHETIC >97% ETB ENDOTHELIN REC EPT
- BQ-788 SODIUM