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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 | Availability | Quantity |
---|---|---|---|
5 mg | $48 | In Stock | |
10 mg | $76 | In Stock | |
25 mg | $160 | In Stock | |
50 mg | $252 | In Stock | |
100 mg | $423 | In Stock | |
1 mL x 10 mM (in DMSO) | $54 | In Stock |
Description | BRL 54443 is a potent 5-HT1E/1F receptor agonist (pKi values: 8.7 and 8.9, respectively). |
Targets&IC50 | 5-HT1D:7.2(pKi), 5-HT1E:8.7(pKi), 5-HT1F:9.25(pKi), 5-HT1B:6.9(pKi), 5-HT1A:7.2(pKi) |
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. |
Alias | 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. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 2 mg/mL (8.68 mM) DMSO: 43 mg/mL (186.7 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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