BQ-123

Names

[ Name ]:
BQ-123

[Synonym ]:
Cyclo(L-α-aspartyl-L-prolyl-D-valyl-L-leucyl-D-tryptophyl)
d-trp-d-asp-pro-d-val-leu
bq-518
MFCD00133204
BQ-123
m.w. 610.70 c31h42n6o7

Biological Activity

[Description]:

BQ-123 is an ETA endothelin receptor antagonist (Ki values are 1.4 and 1500 nM at ETA and ETB receptors respectively) . 1) Reduces ischemia-induced ventricular arrhythmias in a rat model.2) BQ-123 prevents LPS-induced preterm birth in mice via the induction of uterine and placental IL-10.3) The reference for animal injections is 6.7 mg/kg. 4) BQ-123 decreased IL-1β and TNFα in the placenta while also decreasing transcription of ET-1 in the uterus.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Endothelin Receptor

Research Areas >> Infection

[References]

[1]. Olgun NS et al. BQ-123 prevents LPS-induced preterm birth in mice via the induction of uterine and placental IL-10. Toxicol Appl Pharmacol, 2015 Feb 1;282(3):275-84.

[2]. Kanashiro A et al. Cytokines, but not corticotropin-releasing factor and endothelin-1, participate centrally in the febrile response in zymosan-induced arthritis in rats. Brain Res, 2015 Jun 12, 1610:12-9.

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
1053.6±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₃₁H₄₂N₆O₇

[ Molecular Weight ]:
610.701

[ Flash Point ]:
591.0±34.3 °C

[ Exact Mass ]:
610.311523

[ PSA ]:
189.80000

[ LogP ]:
-0.10

[ Vapour Pressure ]:
0.0±0.3 mmHg at 25°C

[ Index of Refraction ]:
1.621

[ Storage condition ]:
-20℃

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Safety Phrases ]:
S22-S24/25

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

A dual role for NOTCH signaling in joint cartilage maintenance and osteoarthritis.

Sci. Signal. 8 , ra71, (2015)

Loss of NOTCH signaling in postnatal murine joints results in osteoarthritis, indicating a requirement for NOTCH during maintenance of joint cartilage. However, NOTCH signaling components are substant...

Subnormothermic ex vivo liver perfusion reduces endothelial cell and bile duct injury after donation after cardiac death pig liver transplantation.

Liver Transpl. 20(11) , 1296-305, (2014)

An ischemic-type biliary stricture (ITBS) is a common feature after liver transplantation using donation after cardiac death (DCD) grafts. We compared sequential subnormothermic ex vivo liver perfusio...

Gene expression profiling and endothelin in acute experimental pancreatitis.

World J. Gastroenterol. 18(32) , 4257-69, (2012)

To analyze gene expression profiles in an experimental pancreatitis and provide functional reversal of hypersensitivity with candidate gene endothelin-1 antagonists.Dibutyltin dichloride (DBTC) is a c...