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 (8)
Reviews (1)
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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
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

Certificate of Analysis / Product Datasheet
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References

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


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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:

Patel et al (2014) Activation of the endothelin system mediates pathological angiogenesis during ischemic retinopathy. J Sex Med 184 3040 PMID: 25203536

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

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

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

Sánchez et al (2014) Endothelin-1 contributes to endothelial dysfunction and enhanced vasoconstriction through augmented superoxide production in penile arteries from insulin-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

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

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


Do you know of a great paper that uses BQ 788 sodium salt from Tocris? Please let us know.

Reviews for BQ 788 sodium salt

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Product works great
By Anonymous on 11/02/2017
Assay Type: Ex Vivo
Species: Mouse

We utilized this product at 1uM to inhibit endothelin-B receptors ex vivo in mouse aortas followed by vasomotor function experiments. We have obtained superior results using this BQ788 product!


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