BQ-788
BQ-788 Basic information
- Product Name:
- BQ-788
- Synonyms:
-
- 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:
- 156161-89-6
- MF:
- C34H52N5NaO7
- MW:
- 665.81
- Product Categories:
-
- Endothelin receptor
- Mol File:
- 156161-89-6.mol
BQ-788 Chemical Properties
- storage temp.
- -20°C
- solubility
- acetonitrile: 0.3 mg/mL
- form
- solid
- color
- white
- Water Solubility
- acetonitrile: 0.3mg/mL
DMSO: 1.2mg/mL
ethanol: 1.2mg/mL
H2O: slightly soluble - InChIKey
- IBWYJVKAVOHKHB-IAZAOAQXNA-N
- SMILES
- C(C1=CN(C(=O)OC)C2=CC=CC=C12)[C@H](C(=O)N[C@@H](C(=O)O)CCCC)NC(=O)[C@H](CC(C)(C)C)NC(N1[C@@H](CCC[C@@H]1C)C)=O.[NaH] |&1:14,18,29,38,42,r|
BQ-788 Usage And Synthesis
Uses
BQ-788 has been used as a selective endothelin-B (ETRB) blocker in human airway smooth muscle cells (HASMCs), uterine mesothelial cells (UtMCs)-derived vascular smooth muscle cells (VSMCs), and human umbilical vein endothelial cells (HUVECs)
Biological Activity
Potent, selective ET B receptor antagonist (IC 50 = 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells).
Biochem/physiol Actions
Selective ETB endothelin receptor antagonist.
in vivo
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[1]. 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[2]. 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[3].
IC 50
ETB
storage
+4°C
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