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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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