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BRL-50481

Name: BRL-50481
Brand: TargetMol
SKU: T5106
Price: 50 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5106Cas No. 433695-36-4

BRL-50481 is a novel and selective PDE7 inhibitor with IC50 values of 0.15 μM for PDE7A, 12.1 μM for PDE7B, 62 μM for PDE4, and 490 μM for PDE3.

BRL-50481

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Purity: 99.66%

Catalog No. T5106Cas No. 433695-36-4

BRL-50481 is a novel and selective PDE7 inhibitor with IC50 values of 0.15 μM for PDE7A, 12.1 μM for PDE7B, 62 μM for PDE4, and 490 μM for PDE3.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$50	In Stock	In Stock
10 mg	$60	In Stock	In Stock
25 mg	$126	In Stock	In Stock
50 mg	$225	In Stock	In Stock
100 mg	$378	In Stock	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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Batch Information

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Purity:99.66%

Appearance:Solid

Color:White

Resource Download

COA LCMS HPLC HNMR

Product Introduction

Bioactivity

Description	BRL-50481 is a novel and selective PDE7 inhibitor with IC50 values of 0.15 μM for PDE7A, 12.1 μM for PDE7B, 62 μM for PDE4, and 490 μM for PDE3.
Targets&IC50	PDE4:62 μM, PDE7B:12 μM, PDE7A:0.15 μM, PDE3:490 μM
In vitro	BRL-50481 marginally increases cAMP levels (19.1±6.2% of the IBMX response at 300 μM) but demonstrates lower potency. At a concentration of 30 μM, BRL-50481 does not independently hinder proliferation but significantly enhances the efficacy of rolipram in this regard. Similarly, it does not affect IL-15-driven proliferation alone, yet amplifies rolipram’s inhibitory properties. A 30-minute pretreatment of human monocytes with BRL-50481 exhibits a minor inhibitory impact (~2 to 10%) on TNFα production across all examined concentrations but boosts the suppressive action of PGE2 on LPS-induced TNFα release. Alone, BRL-50481 has a negligible influence on κB-dependent transcription (5.6±1.9% inhibition at 30 μM) and does not bolster rolipram’s effectiveness (maximum inhibition, 52.9±2.7%; pIC30 value of 5.33±0.12). However, BRL-50481 dose-dependently curtails LPS-induced TNFα secretion in monocytes where PDE7A1 is elevated (21.7±1.6% inhibition at 30 μM after 12 hours) [2].
Cell Research	MOLT-4 cells in 96-well plates are treated for 30 min with BRL-50481. The cAMP content is then determined by an immuno-specific ELISA. Results are expressed as a percentage of the response affected by 100 μM IBMX[2].

Chemical Properties

Molecular Weight	244.27
Formula	C₉H₁₂N₂O₄S
Cas No.	433695-36-4
Smiles	CN(C)S(=O)(=O)c1cc(ccc1C)[N+]([O-])=O
Relative Density.	1.334 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

Ethanol: 20 mg/mL (81.88 mM), Sonication is recommended.

DMSO: 45 mg/mL (184.22 mM), Sonication is recommended.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	4.0938 mL	20.4692 mL	40.9383 mL	204.6915 mL
5 mM	0.8188 mL	4.0938 mL	8.1877 mL	40.9383 mL
10 mM	0.4094 mL	2.0469 mL	4.0938 mL	20.4692 mL
20 mM	0.2047 mL	1.0235 mL	2.0469 mL	10.2346 mL
50 mM	0.0819 mL	0.4094 mL	0.8188 mL	4.0938 mL

DMSO

	1mg	5mg	10mg	50mg
100 mM	0.0409 mL	0.2047 mL	0.4094 mL	2.0469 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