BQ-788 (sodium salt)

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Cat No: 17403

Biochemicals - Receptor Pharmacology

The endothelin (ET) family of proteins mediate a variety of responses, with ET-1 being a potent and long-lasting constrictor of human cardiovascular vessels.{28375} These proteins activate the G protein-coupled receptors ETA and ETB, with ETB being non...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N-[[(2R,6S)-2,6-dimethyl-1-piperidinyl]carbonyl]-4-methyl-L-leucyl-1-(methoxycarbonyl)-D-tryptophyl-D-norleucine, monosodium salt

Correlated keywords:

173326-37-9 1135396-91-6 biochemical receptor antagonist signal transduction vascular disease cardiology BQ788 ETB heart cells binding inhibit inhibitor bind ET1 ET-1 ETA neuroblastoma SK-N-MC SKNMC vasoconstriction bronchoconstriction mediated depressor response

Product Overview:
The endothelin (ET) family of proteins mediate a variety of responses, with ET-1 being a potent and long-lasting constrictor of human cardiovascular vessels.{28375} These proteins activate the G protein-coupled receptors ETA and ETB, with ETB being non-specific for ET protein form.{28375} BQ-788 is a potent, selective antagonist of ETB (IC50 = 1.2 nM for blocking ET-1 binding to human Girardi heart cells).{28374} It weakly inhibits the binding of ET-1 to ETA receptors on human neuroblastoma SK-N-MC cells (IC50 = 1300 nM).{28374} BQ-788 competitively antagonizes the vasoconstriction induced by an ETB-selective agonist on isolated rabbit pulmonary arteries, blocks ET-1 induced bronchoconstriction in guinea pigs, and abolishes an ET-1 mediated depressor response in rats.{28374}

Size	500 µg
Shipping	dry ice
CAS Number	156161-89-6
Molecular Formula	C₃₄H₅₁N₅O₇ • Na
SMILES	C[C@H]1N([C@H](CCC1)C)C(N[C@H](C(N[C@H](CC2=CN(C3=C2C=CC=C3)C(OC)=O)C(N[C@H](CCCC)C(O)=O)=O)=O)CC(C)(C)C)=O.[Na]
Molecular Weight	664,8
Formulation	A solid
Purity	≥95%
Custom Code	3504.00
UNSPSC code	12352100

Technical File

MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.