| Name | BQ-123 |
| Description | BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2. |
| In vitro | In porcine aortic vascular smooth muscle cells, BQ-123 selectively inhibits ETA-mediated contraction. [1] In rat vascular smooth muscle cells, BQ-123 inhibits endothelin-1-induced phosphoinositide breakdown and DNA synthesis. [2] |
| In vivo | In rats, BQ-123 (1 mg/kg, i.v.) ameliorates myocardial ischemic-reperfusion injury. [3] In rats with pentylenetetrazole (PTZ)-induced tonic-clonic seizures, BQ-123 (3 mg/kg, i.v.) potently impedes the formation and spread of seizure. [4] 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. [5] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (8.19 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 12 mg/mL (19.65 mM), Sonication is recommended. DMSO : 250 mg/mL (409.37 mM), Sonication is recommended.
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| Keywords | smooth | pulmonary | pressure | muscle | Inhibitor | inhibit | EndothelinReceptor | Endothelin Receptor | Endothelin A receptor | cells | BQ-123 | BQ 123 | blood | artery |
| Inhibitors Related | BQ-788 | Macitentan | BMS 182874 | Bosentan | BMS 182874 hydrochloride | Sitaxsentan sodium | Edonentan | SB-209670 | Ambrisentan | Sparsentan | Aprocitentan | Clazosentan |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Peptide Compound Library | Inhibitor Library | NO PAINS Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |