BQ 788 sodium salt

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Cat.No. 1500 - BQ 788 sodium salt | C34H50N5NaO7 | CAS No. 156161-89-6
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)
Datasheet
Citations (5)
Reviews
Literature

Biological Activity

Potent, selective ETB receptor antagonist (IC50 = 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells).

Technical Data

M. Wt 663.79
Formula C34H50N5NaO7
Storage Desiccate 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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 3.32 5
ethanol 3.32 5

Preparing Stock Solutions

The following data is based on the product molecular weight 663.79. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.51 mL 7.53 mL 15.07 mL
5 mM 0.3 mL 1.51 mL 3.01 mL
10 mM 0.15 mL 0.75 mL 1.51 mL
50 mM 0.03 mL 0.15 mL 0.3 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: BQ 788 sodium salt, supplier, Selective, ETB, antagonists, Receptors, Endothelin, BQ788, sodium, salt, Endothelin, ETB, Receptors, Endothelin, ETB, Receptors, Tocris Bioscience

5 Citations for BQ 788 sodium salt

Citations are publications that use Tocris products. Selected citations for BQ 788 sodium salt include:

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

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

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

McQueen et al (2007) Endothelin-1 activates ETA receptors to cause reflex scratching in BALB/c mice. Br J Pharmacol 151 278 PMID: 17351652


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