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BRL 44408 Maleate Salt

Name: BRL 44408 Maleate Salt
Brand: TargetMol
SKU: T26904
Price: 68 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T26904Cas No. 681806-46-2

Alias BRL44408 Maleate

BRL 44408 Maleate is a potent α2A-adrenoceptor antagonist with antidepressant and analgesic activity that reduces lipopolysaccharide (LPS)-induced expression and attenuates endogenous lipopolysaccharide-induced acute lung injury through inhibition of the mitogen-activated protein kinase kinase/extracellularly regulated protein kinase signaling pathway in mice.

BRL 44408 Maleate Salt

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Purity: 98.71%

Catalog No. T26904Alias BRL44408 MaleateCas No. 681806-46-2

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$68	-	In Stock
5 mg	$166	-	In Stock
10 mg	$297	-	In Stock
25 mg	$492	-	In Stock
50 mg	$717	-	In Stock
100 mg	$1,056	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:98.71%

Appearance:Solid

Color:Yellow

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

Description	BRL 44408 Maleate is a potent α2A-adrenoceptor antagonist with antidepressant and analgesic activity that reduces lipopolysaccharide (LPS)-induced expression and attenuates endogenous lipopolysaccharide-induced acute lung injury through inhibition of the mitogen-activated protein kinase kinase/extracellularly regulated protein kinase signaling pathway in mice.
Targets&IC50	α2A-adrenoceptor:8.5 nM (Ki), α2A-adrenoceptor:7.9 nM (K (B))
In vitro	BRL 44408 Maleate Salt, a potent (Ki=8.5 nM) and selective (>50-fold) alpha2A-adrenoceptor antagonist (K(B)=7.9 nM). [1]
In vivo	In rats, BRL 44408 Maleate Salt penetrated the central nervous system resulting in peak brain and plasma concentrations of 586 ng/g and 1124 ng/ml, respectively. In a pharmacodynamic assay, pretreatment with BRL 44408 Maleate Salt to rats responding under a fixed-ratio 30 operant response paradigm resulted in a rightward shift of the clonidine dose-response curve, an effect indicative of alpha2-adrenoceptor antagonism in vivo. [1]
Synonyms	BRL44408 Maleate

Chemical Properties

Molecular Weight	331.37
Formula	C₁₇H₂₁N₃O₄
Cas No.	681806-46-2
Smiles	C(=C\C(O)=O)\C(O)=O.CC1C=2C(CN1CC=3NCCN3)=CC=CC2
Relative Density.	no data available

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 20 mg/mL(60.36 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0178 mL	15.0889 mL	30.1777 mL	150.8887 mL
5 mM	0.6036 mL	3.0178 mL	6.0355 mL	30.1777 mL
10 mM	0.3018 mL	1.5089 mL	3.0178 mL	15.0889 mL
20 mM	0.1509 mL	0.7544 mL	1.5089 mL	7.5444 mL
50 mM	0.0604 mL	0.3018 mL	0.6036 mL	3.0178 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc