BRL-50481

Name: BRL-50481
Brand: MedChemExpress
SKU: HY-109586
Rating: 5.0 (4 reviews)

Art. -Nr.: HY-109586 Reinheit: 99.81%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

BRL-50481 is a novel and selective inhibitor of PDE7 with IC₅₀s of 0.15, 12.1, 62 and 490 μM for PDE7A, PDE7B, PDE4 and PDE3, respectively.

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BRL-50481 Chemische Struktur

CAS. Nr. : 433695-36-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
Solid
5 mg	Auf Lager	Estimated Time of Arrival: December 31
10 mg	Auf Lager	Estimated Time of Arrival: December 31
25 mg	Auf Lager	Estimated Time of Arrival: December 31
50 mg	Auf Lager	Estimated Time of Arrival: December 31
100 mg	Auf Lager	Estimated Time of Arrival: December 31
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500 mg	Angebot einholen

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This product is a controlled substance and not for sale in your territory.

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Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE BRL-50481

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

Biologische Aktivität
Protokoll
Reinheit & Dokumentation
Verweise
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Beschreibung

BRL-50481 is a novel and selective inhibitor of PDE7 with IC₅₀s of 0.15, 12.1, 62 and 490 μM for PDE7A, PDE7B, PDE4 and PDE3, respectively.

IC₅₀ & Target

PDE7

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	2.2 μM Compound: BRL-50481	Inhibition of human recombinant PDE7A1 expressed in baculovirus-infected insect Sf9 cells by modified two-step method Inhibition of human recombinant PDE7A1 expressed in baculovirus-infected insect Sf9 cells by modified two-step method	[PMID: 19303290]

In Vitro

BRL-50481 increases the cAMP content (19.1±6.2% of IBMX response at 300 μM) but is considerably less potent. BRL-50481 (30 μM) fails to suppress proliferation by itself but significantly potentiates the effect of rolipram. BRL-50481 (30 μM) has no effect on IL-15-induced proliferation but augments the inhibitory effect of rolipram. Pretreatment (30 min) of human monocytes with BRL-50481 has, by itself, a negligible (~2 to 10%) inhibitory effect on TNFα output at all concentrations tested. BRL-50481 also potentiates the inhibitory effect of PGE₂ on LPS-induced TNFα release. BRL-50481 has no significant effect by itself on κB-dependent transcription (5.6±1.9% inhibition at 30 μM) and fails to enhance the effect of rolipram (maximum inhibition, 52.9±2.7%; pIC₃₀ value of 5.33±0.12). BRL-50481 suppresses, in a concentration-dependent manner, LPS-induced TNFα release in monocytes in which PDE7A1 is induced (21.7±1.6% inhibition at 30 μM at the 12-h time point)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molekulargewicht

244.27

Formel

C₉H₁₂N₂O₄S

CAS. Nr.

433695-36-4

Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC([N+]([O-])=O)=CC=C1C)(N(C)C)=O

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (409.38 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.0938 mL	20.4692 mL	40.9383 mL
5 mM	0.8188 mL	4.0938 mL	8.1877 mL
10 mM	0.4094 mL	2.0469 mL	4.0938 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner
Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Reinheit & Dokumentation

Purity: 99.81%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (250 KB) HNMR (173 KB) LCMS (103 KB)

Handling Instructions (2659 KB)

Verweise

[1]. Safavi M, et al. New methods for the discovery and synthesis of PDE7 inhibitors as new drugs for neurologicaland inflammatory disorders. Expert Opin Drug Discov. 2013 Jun;8(6):733-51. [Content Brief]

[2]. Smith SJ, et al. Discovery of BRL 50481 [3-(N,N-dimethylsulfonamido)-4-methyl-nitrobenzene], a selective inhibitor of phosphodiesterase 7: in vitro studies in human monocytes, lung macrophages, and CD8+ T-lymphocytes. Mol Pharmacol. 2004 Dec;66(6):1679-89. [Content Brief]

Zellassay
^[2]

MOLT-4 cells in 96-well plates are treated for 30 min with BRL-50481 as indicated. The cAMP content is then determined by an immunospecific ELISA. Results are expressed as a percentage of the response affected by 100 μM IBMX^[2].

MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.

Verweise

[1]. Safavi M, et al. New methods for the discovery and synthesis of PDE7 inhibitors as new drugs for neurologicaland inflammatory disorders. Expert Opin Drug Discov. 2013 Jun;8(6):733-51. [Content Brief]

[2]. Smith SJ, et al. Discovery of BRL 50481 [3-(N,N-dimethylsulfonamido)-4-methyl-nitrobenzene], a selective inhibitor of phosphodiesterase 7: in vitro studies in human monocytes, lung macrophages, and CD8+ T-lymphocytes. Mol Pharmacol. 2004 Dec;66(6):1679-89. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	4.0938 mL	20.4692 mL	40.9383 mL	102.3458 mL
	5 mM	0.8188 mL	4.0938 mL	8.1877 mL	20.4692 mL
	10 mM	0.4094 mL	2.0469 mL	4.0938 mL	10.2346 mL
	15 mM	0.2729 mL	1.3646 mL	2.7292 mL	6.8231 mL
	20 mM	0.2047 mL	1.0235 mL	2.0469 mL	5.1173 mL
	25 mM	0.1638 mL	0.8188 mL	1.6375 mL	4.0938 mL
	30 mM	0.1365 mL	0.6823 mL	1.3646 mL	3.4115 mL
	40 mM	0.1023 mL	0.5117 mL	1.0235 mL	2.5586 mL
	50 mM	0.0819 mL	0.4094 mL	0.8188 mL	2.0469 mL
	60 mM	0.0682 mL	0.3412 mL	0.6823 mL	1.7058 mL
	80 mM	0.0512 mL	0.2559 mL	0.5117 mL	1.2793 mL
	100 mM	0.0409 mL	0.2047 mL	0.4094 mL	1.0235 mL

BRL-50481 Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BRL-50481433695-36-4BRL50481BRL 50481Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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BRL-50481

Kundenbewertung

BRL-50481 Related Antibodies

4 Publications Citing Use of MCE BRL-50481

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen:

Biologische Aktivität

Protokoll

Reinheit & Dokumentation

Verweise

Kundenbewertung

BRL-50481 Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

BRL-50481 Related Classifications

Keywords:

Ihre kürzlich angesehenen Produkte:

Kundenbewertung

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SAFETY DATA SHEET (SDS)

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