BRL-54443

Catalog No.S2852

BRL-54443 Chemical Structure

Molecular Weight(MW): 230.31

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.

Size Price Stock Quantity  
In DMSO USD 120 In stock
USD 90 In stock
USD 370 In stock
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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

Animal Research:[1]
+ Expand
  • Animal Models: Adult male cats
  • Formulation: Distilled water containing 1 equivalent 2,3-dihydroxybutanedioic acid+0.9% NaCl
  • Dosages: 3 μg/kg-30 mg/kg
  • Administration: s.c.
    (Only for Reference)

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(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30 mg/mL

* 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.

Chemical Information

Molecular Weight 230.31
Formula

C14H18N2O

CAS No. 57477-39-1
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID