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BQ-123 is a selective endothelin A receptors (ETAR) antagonist with an IC50 value of 7.3 nM, Ki values are 1.4 and 1500 nM at ETA and ETB receptors respectively. 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.
In vivo, BQ-123 (3 mg/kg, i.v.) potently impedes the formation and spread of seizure in rats with pentylenetetrazole (PTZ)-induced tonic-clonic seizures. 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.
| Molecular Weight | 610.7 |
| Formula | C31H42N6O7 |
| CAS Number | 136553-81-6 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Endothelin Receptor Products |
|---|
| Zibotentan
Zibotentan (ZD4054) is a more selective and specific endothelin-A receptor (ETAR) antagonist with an IC50 value of 21 nM. |
| Ambrisentan
Ambrisentan is an orally active, highly selective antagonist of the endothelin-1 type A receptor. |
| Sitaxsentan sodium
Sitaxsentan (TBC-11251) is an orally active, highly selective antagonist of endothelin A receptors. |
| Macitentan
Macitentan is an orally-active, tissue-targeting dual ET receptor antagonist. |
| Bosentan Hydrate
Bosentan is an endothelin (ET) receptors antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. |
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Products are for research use only. Not for human use. We do not sell to patients.
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