[CAS NO. 136553-81-6] BQ-123

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PRODUCTS SPECIFICATIONS [136553-81-6]

Catalog

SLK-S7883

Brand

Selleck

CAS

136553-81-6

DESCRIPTION [136553-81-6]

Overview

MDL	MFCD00133204
Molecular Weight	610.7
Molecular Formula	C31H42N6O7
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

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.6375 mL	8.1873 mL	16.3747 mL
5 mM	0.3275 mL	1.6375 mL	3.2749 mL
10 mM	0.1637 mL	0.8187 mL	1.6375 mL
50 mM	0.0327 mL	0.1637 mL	0.3275 mL

Description

BQ-123 is a selective antagonist with of 7.3 nM. Phase 2.

Targets

Endothelin A receptor ^[1]
(Cell-free assay)

7.3 nM

In vitro

In porcine aortic vascular smooth muscle cells, BQ-123 selectively inhibits ETA-mediated contraction. In rat vascular smooth muscle cells, BQ-123 inhibits endothelin-1-induced phosphoinositide breakdown and DNA synthesis.

In vivo

In rats, BQ-123 (1 mg/kg, i.v.) ameliorates myocardial ischemic-reperfusion injury. In rats with pentylenetetrazole (PTZ)-induced tonic-clonic seizures, BQ-123 (3 mg/kg, i.v.) potently impedes the formation and spread of seizure. In pregnant C57BL/6 mice, BQ-123 (6.7 mg/kg, i.p.) prevents LPS-induced preterm birth in mice via the induction of uterine and placental IL-10.

References

[1] Ihara M, et al. J Cardiovasc Pharmacol. 1992, 12, S11-14.
[2] Eguchi S, et al. FEBS Lett. 1992, 302(3), 243-246.
[3] Goyal SN, et al. Biomed Pharmacother. 2010, 64(9), 639-646.
[4] Erdogan H, et al. Hum Exp Toxicol. 2014, 33(10), 1008-1016.
[5] Olgun NS, et al. Toxicol Appl Pharmacol. 2015, 282(3), 275-284.