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BRL-54443 5-HT Receptor agonist

Name: BRL-54443
Brand: Selleck Chemicals
SKU: S2852
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S2852

BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pK_i of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.

Chemical Structure

Molecular Weight: 230.31

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S285201 DMSO]46 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false Purity: 99.94%

99.94

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Chemical Information, Storage & Stability

Molecular Weight	230.31	Formula	C₁₄H₁₈N₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	57477-39-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CN1CCC(CC1)C2=CNC3=C2C=C(C=C3)O

Solubility

In vitro
Batch:

DMSO : 46 mg/mL ( (199.73 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%propylene glycol 1 5%Tween80 2 65%D5W Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (130.26mM)	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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	5-HT1F ^[1] 9.25(pKi) 5-HT1E ^[1] 8.7(pKi) 5-HT1A ^[1] 7.2(pKi) 5-HT1D ^[1] 7.2(pKi) 5-HT1B ^[1] 6.9(pKi)
In vitro	BRL 54443 has also measurable affinity for the 5-HT_2A receptor. BRL 54443 induces contraction with a −logEC50 of 6.52. Contraction caused by BRL 54443 is likely mediated through stimulation of 5-HT5-HT_2A receptors. ^[2]
In vivo	BRL 54443 induces an immediate dose-dependent maximal intragastric volume increase vs. saline. ^[1]
References	https://pubmed.ncbi.nlm.nih.gov/15178373/ https://pubmed.ncbi.nlm.nih.gov/11259531/

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