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| 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 | | EINECS: | | | 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| |
| WGK Germany | 3 | | Storage Class | 11 - Combustible Solids |
| | 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 |
| | BQ-788 Preparation Products And Raw materials |
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