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BQ-123

$100$420

Products Details

Product Description

– BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension[1][2][3].

Web ID

– HY-12378

Storage Temperature

– -80°C, 2 years; -20°C, 1 year (Powder, sealed storage, away from moisture and light)

Shipping

– Blue Ice

Applications

– COVID-19-immunoregulation

Molecular Formula

– C31H42N6O7

References

– [1]Ihara M, et al. In vitro biological profile of a highly potent novel endothelin (ET) antagonist BQ-123 selective for the ETA receptor. J Cardiovasc Pharmacol. 1992;20 Suppl 12:S11-S14.|[2]Sakamoto A, et al. Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonist and endothelinB-selective agonists. J Biol Chem. 1993 Apr 25;268(12):8547-53.|[3]Erdogan H et al. The protective effects of endothelin-A receptor antagonist BQ-123 in pentylenetetrazole-induced seizure in rats. Hum Exp Toxicol, 2014 Oct, 33(10):1008-16.|[4]Zamora MA, et al. BQ123, an ETA receptor antagonist, inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells. Am J Respir Cell Mol Biol. 1993;9(4):429-433.|[5]Douglas SA, et al. BQ-123, a selective endothelin subtype A-receptor antagonist, lowers blood pressure in different rat models of hypertension. J Hypertens. 1994;12(5):561-567.

CAS Number

– 136553-81-6

Molecular Weight

– 610.70

Compound Purity

– 99.78

SMILES

– O=C(N[C@](C(N(CCC1)[C@]1([H])C2=O)=O)([H])CC(O)=O)[C@H](NC([C@@H](NC([C@H](N2)C(C)C)=O)CC(C)C)=O)CC3=CNC4=CC=CC=C34

Clinical Information

– Phase 4

Research Area

– Cardiovascular Disease

Solubility

– DMSO : 50 mg/mL (ultrasonic)

Target

– Endothelin Receptor

Isoform

– ETA

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.

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