product name BQ-123
Description: BQ-123 is a potentr and selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. BQ123 potentiates acetaminophen induced hypothermia and reduces infarction following focal cerebral ischemia in rats. BQ123 Stimulates Skeletal Muscle Antioxidant Defense via Nrf2 Activation in LPS-Treated Rats. BQ123 reduces pulmonary vascular resistance after surgical intervention for congenital heart disease. BQ123 protects against myocardial and endothelial reperfusion injury.
References: J Cardiovasc Pharmacol. 1992;20 Suppl 12:S11-4; FEBS Lett. 1992 May 18;302(3):243-6; Biomed Pharmacother. 2010 Nov;64(9):639-46.
610.7
Formula
C31H42N6O7
CAS No.
136553-81-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (163.7 mM)
Water: <1 mg/mL
Ethanol: 15 mg/mL (24.6 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19417231
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: In the ETA-expressing cells, BQ123 (10-6 M) inhibited endothelin-1 (ET-1) (10-6 M)-induced [Ca2+]i increase by 95%. In rat vascular smooth muscle cells (VSMC), BQ-123 inhibited ET-1 receptor binding, cellular contraction, [Ca2+ ]i mobilization, [3H]thymidine incorporation, MAP kinase activation and MTT reduction induced by ET-1. However, BQ-123 didn’t inhibit angiotensin II (Ang II)- and arginine vasopressin (AVP)-induced increases in MAP kinase activity and [Ca2+]i mobilization |
|---|---|
| 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 |
| Animal model | Male Wistar rats |
| Formulation & Dosage | Dissolved in 5% NaHCO3; 1 mg/kg; i.v. injection |
| References | J Cardiovasc Pharmacol. 1992;20 Suppl 12:S11-4; FEBS Lett. 1992 May 18;302(3):243-6; Biomed Pharmacother. 2010 Nov;64(9):639-46. |
