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BRL 54443 is a potent 5-HT1E/1F receptor agonist (pKi values: 8.7 and 8.9, respectively).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $40 | In Stock | In Stock | |
| 10 mg | $68 | In Stock | In Stock | |
| 25 mg | $147 | In Stock | In Stock | |
| 50 mg | $247 | In Stock | In Stock | |
| 100 mg | $367 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $44 | In Stock | In Stock |
| Description | BRL 54443 is a potent 5-HT1E/1F receptor agonist (pKi values: 8.7 and 8.9, respectively). |
| Targets&IC50 | 5-HT1A:7.2(pKi), 5-HT1D:7.2(pKi), 5-HT2A receptor:1259 nM (Ki), 5-HT2B receptor:100 nM (Ki), 5-HT1F:9.25(pKi), 5-HT7 receptor:>10,000 nM (Ki), 5-HT1E:8.7(pKi), 5-HT6 receptor:>10,000 nM (Ki), 5-HT1B:6.9(pKi), 5-HT2C receptor:316 nM (Ki) |
| In vitro | BRL 54443 induced contractions with a -logEC50 of 6.52. Contractions induced by BRL 54443 are likely mediated by stimulation of 5-HT 5-HT 2A receptors. |
| In vivo | BRL 54443 induced contractions with a -logEC50 of 6.52. Contractions induced by BRL 54443 are likely mediated by stimulation of 5-HT 5-HT 2A receptors. |
| Kinase Assay | In Vitro Radiometric PKD Kinase Assay: The radiometric kinase assay is carried out by coincubating 0.5 μCi of [γ-32P]ATP, 20 μM ATP, 50 ng of purified recombinant human PKD (PKD1, PKD2, and PKD3) or CAMKIIα proteins, and 2.5 μg of Syntide-2 in 50 μl of kinase buffer that contains 50 mM Tris-HCl, pH 7.5, 4 mM MgCl2, 10 mM β-mercaptoethanol. The reaction is carried out under conditions that the initial rate is within the linear kinetic range. The filter papers are then washed three times in 0.5% phosphoric acid, air-dried, and counted using a Beckman LS6500 multipurpose scintillation counter. |
| Synonyms | BRL54443 |
| Molecular Weight | 230.31 |
| Formula | C14H18N2O |
| Cas No. | 57477-39-1 |
| Smiles | OC=1C=C2C(=CNC2=CC1)C3CCN(C)CC3 |
| Relative Density. | 1.196 g/cm3 |
| Storage | 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: 2 mg/mL (8.68 mM), Sonication is recommended. DMSO: 43 mg/mL (186.7 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (8.68 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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