BRL-50481

This product is for research use only, not for human use. We do not sell to patients.

BRL-50481
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250mg$450Check With Us
500mg$750Check With Us
1g$1125Check With Us

Cat #: V4092 CAS #: 433695-36-4 Purity ≥ 98%

Description: BRL-50481 is a novel, potent and selective inhibitor of phosphodiesterase 7 (PDE7) with IC50s of 0.15, 12.1, 62 and 490 μM for PDE7A, PDE7B, PDE4 and PDE3, respectively.

References: 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.

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Molecular Weight (MW)244.27
Molecular FormulaC9H12N2O4S
CAS No.433695-36-4
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: ≥ 45mg/mLr
Water: < 1mg/mLr
Ethanol: N/A
SMILES CodeO=S(C1=CC([N+]([O-])=O)=CC=C1C)(N(C)C)=O
SynonymsBRL-50481; BRL 50481; BRL50481
ProtocolIn VitroBRL-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).
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM4.0938 mL20.4692 mL40.9383 mL81.8766 mL
5mM0.8188 mL4.0938 mL8.1877 mL16.3753 mL
10mM0.4094 mL2.0469 mL4.0938 mL8.1877 mL
20mM0.2047 mL1.0235 mL2.0469 mL4.0938 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.