BQ-123

CAT: 0804-HY-12378-01Size: 1 mgDry Ice: NoHazardous: No
CAT#:0804-HY-12378-01Size:1 mg
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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].
CAS Number
[136553-81-6]
UNSPSC
12352209
Hazard Statement
H302, H315, H319, H335
Target
Endothelin Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein
Applications
COVID-19-immunoregulation
Field of Research
Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/BQ-123.html
Purity
99.82
Solubility
DMSO : 50 mg/mL (ultrasonic)
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
Molecular Formula
C31H42N6O7
Molecular Weight
610.70
Precautions
H302, H315, H319, H335
References & Citations
[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.
Shipping Conditions
Blue Ice
Storage Conditions
-80°C, 2 years; -20°C, 1 year (Powder, sealed storage, away from moisture and light)
Scientific Category
Reference compound1
Clinical Information
Phase 4
Isoform
ETA

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