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BQ-788
$180 – $600
Products Details
Product Description
– BQ-788 is a potent, selective ETB receptor antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC50 of 1300 nM[1].
Web ID
– HY-15894A
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Metabolism-sugar/lipid metabolism
Molecular Formula
– C34H51N5O7
Citations
– Cells. 2021, 10(11), 3072.|Environ Pollut. 2016 Feb;209:11-20.|Environ Pollut. 2016 Nov;218:487-496. |Neurotherapeutics. 2021 Oct 18.|Toxicol Sci. 2016 Jan;149(1):213-26.|BMC Cancer. 2018 Feb 6;18(1):154.|Environ Sci Pollut Res Int. 2018 May;25(15):14713-14725.|PLoS Pathog. 2020 Oct 19;16(10):e1008947.
References
– [1]Sargent CA, et al. Effect of endothelin antagonists with or without BQ 788 on ET-1 responses in pithed rats. J Cardiovasc Pharmacol. 1995;26 Suppl 3:S216-8.|[2]Okada M, et al. BQ-788, a selective endothelin ET(B) receptor antagonist. Cardiovasc Drug Rev. 2002 Winter;20(1):53-66.|[3]Fattori V, et al. Differential regulation of oxidative stress and cytokine production by endothelin ETA and ETB receptors in superoxide anion-induced inflammation and pain in mice. J Drug Target. 2016 Oct 5:1-27
CAS Number
– 173326-37-9
Molecular Weight
– 641.80
Compound Purity
– 98.28
SMILES
– CCCC[C@H](C(O)=O)NC([C@@H](CC1=CN(C(OC)=O)C2=CC=CC=C12)NC([C@H](CC(C)(C)C)NC(N3[C@H](C)CCC[C@@H]3C)=O)=O)=O
Clinical Information
– Phase 1
Research Area
– Cardiovascular Disease; Endocrinology
Solubility
– DMSO : 170 mg/mL (ultrasonic;warming;heat to 60°C)
Target
– Endothelin Receptor
Isoform
– ETB
Pathway
– GPCR/G Protein
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
