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BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $80 | In Stock | In Stock | |
| 5 mg | $213 | In Stock | In Stock | |
| 10 mg | $347 | In Stock | In Stock | |
| 25 mg | $577 | In Stock | In Stock | |
| 50 mg | $823 | In Stock | In Stock | |
| 100 mg | $1,090 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $288 | In Stock | In Stock |
| Description | BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2. |
| Targets&IC50 | ETA receptor:7.3 nM |
| 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] |
| Synonyms | BQ123 |
| Molecular Weight | 610.7 |
| Formula | C31H42N6O7 |
| Cas No. | 136553-81-6 |
| Smiles | [H][C@@]12CCCN1C(=O)[C@@]([H])(CC(O)=O)NC(=O)[C@@H](Cc1c[nH]c3ccccc13)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC2=O)C(C)C |
| Relative Density. | 1.33 g/cm3 (Predicted) |
| Color | White |
| Appearance | Solid |
| Sequence | Cyclo(d-Asp-Pro-d-Val-Leu-d-Trp) |
| Sequence Short | Cyclo(d-DP-d-VL-d-W) |
| Storage | keep away from moisture,keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 12 mg/mL (19.65 mM), Sonication is recommended. DMSO: 93 mg/mL (152.28 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (8.19 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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