Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C34H50N5O7.Na |
Molecular Weight | 663.7799 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 5 / 5 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[Na+].CCCC[C@@H](NC(=O)[C@@H](CC1=CN(C(=O)OC)C2=C1C=CC=C2)NC(=O)[C@H](CC(C)(C)C)NC(=O)N3[C@@H](C)CCC[C@H]3C)C([O-])=O
InChI
InChIKey=QCVIFBRTTLMEOV-FUKQNADPSA-M
InChI=1S/C34H51N5O7.Na/c1-8-9-16-25(31(42)43)35-29(40)26(18-23-20-38(33(45)46-7)28-17-11-10-15-24(23)28)36-30(41)27(19-34(4,5)6)37-32(44)39-21(2)13-12-14-22(39)3;/h10-11,15,17,20-22,25-27H,8-9,12-14,16,18-19H2,1-7H3,(H,35,40)(H,36,41)(H,37,44)(H,42,43);/q;+1/p-1/t21-,22+,25-,26-,27+;/m1./s1
BQ-788, a selective endothelin (ET) B-receptor antagonist, was developed by Banyu. This compound is widely used to demonstrate the role of ET-1 and ET(B) receptor subtypes in physiological and/or pathophysiological conditions. BQ-788 was studied against hypertension. However, this study was discontinued. Besides, was shown that BQ788 could protect against brain edema by inhibiting vascular endothelial growth factor-A-mediated decrease in claudin-5. The intralesional applications of BQ788 were well tolerated and showed signs of directly and indirectly reducing the viability of melanoma cells.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL1785 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12070534 |
1.2 nM [IC50] |
PubMed
Title | Date | PubMed |
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Endothelin-1 binding to endothelin receptors in the rat anterior pituitary gland: possible formation of an ETA-ETB receptor heterodimer. | 2002 Apr |
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Actions of endothelin and corticotropin releasing factor in the guinea-pig ileum: no evidence for an interaction with capsaicin-sensitive neurons. | 2003 Aug |
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Ventricular nonmyocytes inhibit doxorubicin-induced myocyte apoptosis: involvement of endogenous endothelin-1 as a paracrine factor. | 2004 May |
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Endothelins induce ETB receptor-mediated mechanical hypernociception in rat hindpaw: roles of cAMP and protein kinase C. | 2004 Oct 6 |
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Role of ET(A) and ET(B) endothelin receptors on endothelin-1-induced potentiation of nociceptive and thermal hyperalgesic responses evoked by capsaicin in rats. | 2009 Jul 3 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26330458
Three patients received a single intralesional BQ788 application of 3 mg
Route of Administration:
Other
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FDA ORPHAN DRUG |
506215
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44OLL8XEJ4
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16759603
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156161-89-6
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BQ-788
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DTXSID40166053
Created by
admin on Fri Dec 15 18:04:58 GMT 2023 , Edited by admin on Fri Dec 15 18:04:58 GMT 2023
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ACTIVE MOIETY
SUBSTANCE RECORD