N-CIS-2,6-DIMETHYLPIPERIDINOCARBONYL-BETA-TBU-ALA-D-TRP(1-METHOXYCARBONYL)-D-NLE-OH
- Product Name
- N-CIS-2,6-DIMETHYLPIPERIDINOCARBONYL-BETA-TBU-ALA-D-TRP(1-METHOXYCARBONYL)-D-NLE-OH
- CAS No.
- 173326-37-9
- Chemical Name
- N-CIS-2,6-DIMETHYLPIPERIDINOCARBONYL-BETA-TBU-ALA-D-TRP(1-METHOXYCARBONYL)-D-NLE-OH
- Synonyms
- BQ788,BQ 788;BQ788, CID 3081333;N-cis-2,6-DiMethylpiperidinocarbonyl-b-tBu-Ala-D-Trp(1-Methoxycarbonyl)-D-Nle-OH;D-Norleucine, N-[(cis-2,6-dimethyl-1-piperidinyl)carbonyl]-4-methyl-L-leucyl-1-(methoxycarbonyl)-D-tryptophyl- (9CI);D-Norleucine,N-[N-[N-[(2,6-dimethyl-1-piperidinyl)carbonyl]-4-methyl-L-leucyl]-1-(methoxycarbonyl)-D-tryptophyl]-,cis-;(2R)-2-[[(2R)-2-[[(2S)-2-[[(2R,6S)-2,6-dimethylpiperidine-1-carbonyl]amino]-4,4-dimethylpentanoyl]amino]-3-(1-methoxycarbonylindol-3-yl)propanoyl]amino]hexanoicacid;(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]HEXANOIC ACID
- CBNumber
- CB41474659
- Molecular Formula
- C34H51N5O7
- Formula Weight
- 641.8
- MOL File
- 173326-37-9.mol
N-CIS-2,6-DIMETHYLPIPERIDINOCARBONYL-BETA-TBU-ALA-D-TRP(1-METHOXYCARBONYL)-D-NLE-OH Property
- Density
- 1.23±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 10 mM
- form
- A solid
- pka
- 3.40±0.10(Predicted)
N-Bromosuccinimide Price
- Product number
- FB108685
- Product name
- BQ-788
- Packaging
- 500ug
- Price
- $400
- Updated
- 2021/12/16
- Product number
- FB108685
- Product name
- BQ-788
- Packaging
- 1mg
- Price
- $600
- Updated
- 2021/12/16
- Product number
- FB108685
- Product name
- BQ-788
- Packaging
- 2mg
- Price
- $1100
- Updated
- 2021/12/16
- Product number
- 9131CN
- Product name
- BQ-788freeacid
- Packaging
- 2mg
- Price
- $1535
- Updated
- 2021/12/16
- Product number
- FB108685
- Product name
- BQ-788
- Packaging
- 5mg
- Price
- $2600
- Updated
- 2021/12/16
N-CIS-2,6-DIMETHYLPIPERIDINOCARBONYL-BETA-TBU-ALA-D-TRP(1-METHOXYCARBONYL)-D-NLE-OH Chemical Properties,Usage,Production
Biological Activity
BQ-788 is a potent and selective ETB receptor antagonist with IC50 of 1.2 nM for inhibiting ET-1 binding to the ETB receptor in human Girrardi heart cells.
in vitro
BQ-788 potently and competitively inhibits 125 I-labeled ET-1 binding to ETB receptors in human Girardi heart cells (hGH) 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.
in vivo
BQ-788 (3 mg/kg/h, iv) completely inhibits a pharmacological dose of ET-1- or sarafotoxin6c (0.5 nmol/kg, iv)-induced ETB receptor-mediated depressor, but not pressor responses in conscious rats. Furthermore, BQ-788 markedly increased 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, iv) 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, intra plantar 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 decreases peroxidation, respectively.
target
IC50: 1.2 nM (ETB)
N-CIS-2,6-DIMETHYLPIPERIDINOCARBONYL-BETA-TBU-ALA-D-TRP(1-METHOXYCARBONYL)-D-NLE-OH Preparation Products And Raw materials
Raw materials
Preparation Products
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