BRL-54443

Catalog No.S2852 Batch:S285201

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Technical Data

Formula

C14H18N2O
Molecular Weight 230.31 CAS No. 57477-39-1
Solubility (25°C)* In vitro DMSO 46 mg/mL (199.73 mM)
Ethanol 2 mg/mL (8.68 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
30%propylene glycol 5%Tween80 65%D5W
30.0mg/ml Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.
Targets
5-HT1F [1] 5-HT1E [1] 5-HT1A [1] 5-HT1D [1] 5-HT1B [1]
9.25(pKi) 8.7(pKi) 7.2(pKi) 7.2(pKi) 6.9(pKi)
In vitro BRL 54443 has also measurable affinity for the 5-HT2A receptor. BRL 54443 induces contraction with a −logEC50 of 6.52. Contraction caused by BRL 54443 is likely mediated through stimulation of 5-HT5-HT2A receptors. [2]
In vivo BRL 54443 induces an immediate dose-dependent maximal intragastric volume increase vs. saline. [1]

Protocol (from reference)

Animal Study:[1]
  • Animal Models

    Adult male cats

  • Dosages

    3 μg/kg-30 mg/kg

  • Administration

    s.c.

Selleck's BRL-54443 has been cited by 2 publications

Degradome analysis to identify direct protein substrates of small-molecule degraders [ bioRxiv, 2024, 10.1101/2024.01.28.577572] PubMed: none
Serotonin/HTR1E signaling blocks chronic stress-promoted progression of ovarian cancer [ Theranostics, 2021, 11(14):6950-6965] PubMed: 34093864

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.