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Submit ReviewBQ 788 sodium salt
Description: Selective ETB antagonist
Chemical Name: N-[(cis-2,6-Dimethyl-1-piperidinyl)carbonyl]-4-methyl-L-leucyl-1-(methoxycarbonyl)-D-tryptophyl-D-norleucine sodium salt
Purity: ≥95% (HPLC)
Biological Activity for BQ 788 sodium salt
BQ 788 sodium salt is a potent, selective ETB receptor antagonist (IC50 = 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells).
Technical Data for BQ 788 sodium salt
| M. Wt | 663.79 |
| Formula | C34H50N5NaO7 |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 156161-89-6 |
| PubChem ID | 16759603 |
| InChI Key | QCVIFBRTTLMEOV-FUKQNADPSA-M |
| 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)N1[C@@H](C)CCC[C@H]1C)C([O-])=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for BQ 788 sodium salt
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 3.32 | 5 |
Preparing Stock Solutions for BQ 788 sodium salt
The following data is based on the product molecular weight 663.79. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.05 mM | 30.13 mL | 150.65 mL | 301.3 mL |
| 0.25 mM | 6.03 mL | 30.13 mL | 60.26 mL |
| 0.5 mM | 3.01 mL | 15.07 mL | 30.13 mL |
| 2.5 mM | 0.6 mL | 3.01 mL | 6.03 mL |
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Product Datasheets for BQ 788 sodium salt
References for BQ 788 sodium salt
References are publications that support the biological activity of the product.
Davenport (2002) International Union of Pharmacology. XXIX. Update on endothelin receptor nomenclature. Pharmacol.Rev. 54 219 PMID: 12037137
Ishikawa et al (1994) Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proc.Natl.Acad.Sci.U.S.A. 91 4892 PMID: 8197152
Okada and Nishikibe (2002) BQ-788, a selective endothelin ETB receptor antagonist. Cardiovasc.Drug Rev. 20 53 PMID: 12070534
If you know of a relevant reference for BQ 788 sodium salt, please let us know.
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Keywords: BQ 788 sodium salt, BQ 788 sodium salt supplier, Selective, ETB, antagonists, Receptors, Endothelin, BQ788, sodium, salt, 1500, Tocris Bioscience
8 Citations for BQ 788 sodium salt
Citations are publications that use Tocris products. Selected citations for BQ 788 sodium salt include:
Yeligar et al (2009) Ethanol-induced expression of ET-1 and ET-BR in liver sinusoidal endothelial cells and human endothelial cells involves hypoxia-inducible factor-1alpha and microrNA-199. J Immunol 183 5232 PMID: 19783678
Durgan et al (2015) Increased cerebrovascular sensitivity to endothelin-1 in a rat model of obstructive sleep apnea: a role for endothelin receptor B. J Cereb Blood Flow Metab 35 402 PMID: 25425077
Sutcliffe et al (2009) Transcriptional regulation of monocyte chemotactic protein-1 release by endothelin-1 in human airway smooth muscle cells involves NF-kappaB and AP-1. Br J Pharmacol 157 436 PMID: 19371341
Patel et al (2014) Activation of the endothelin system mediates pathological angiogenesis during ischemic retinopathy. J Sex Med 184 3040 PMID: 25203536
Allahdadi et al (2010) Endothelin-1 induces contraction of female rat internal pudendal and clitoral arteries through ET(A) receptor and rho-kinase activation. PLoS One 7 2096 PMID: 20412427
McQueen et al (2007) Endothelin-1 activates ETA receptors to cause reflex scratching in BALB/c mice. Br J Pharmacol 151 278 PMID: 17351652
Sánchez et al (2014) Endothelin-1 contributes to endothelial dysfunction and enhanced vasoconstriction through augmented superoxide production in penile arteries from Ins-resistant obese rats: role of ET(A) and ET(B) receptors. Br J Pharmacol 171 5682 PMID: 25091502
Ou et al (2014) Adaptive regulation of endothelin receptor type-A and type-B in vascular smooth muscle cells during pregnancy in rats. J Cell Physiol 229 489 PMID: 24105843
Do you know of a great paper that uses BQ 788 sodium salt from Tocris? Please let us know.
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