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Preladenant (MK-3814; SCH420814)

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Preladenant (MK-3814; SCH420814)
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Cat #: V3944 CAS #: 377727-87-2 Purity ≥ 98%

Description: Preladenant (formerly known as MK-3814; SCH-420814) is a novel potent, selective and competitive antagonist of adenosine A2A receptor with potential immunomodulatory effects and may be used for the treatment for Parkinson's disease.

References: Hodgson RA, et al. Characterization of the potent and highly selective A2A receptor antagonists preladenant and SCH 412348 [7-[2-[4-2,4-difluorophenyl]-1-piperazinyl]ethyl]-2-(2-furanyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine] in rodent

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Molecular Weight (MW)503.57
Molecular FormulaC25H29N9O3
CAS No.377727-87-2
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 10 mMr
Water: N/Ar
Ethanol: N/A
SMILES CodeNC1=NC(N(CCN2CCN(C3=CC=C(OCCOC)C=C3)CC2)N=C4)=C4C5=NC(C6=CC=CO6)=NN15
SynonymsSCH420814; MK 3814; SCH-420814; MK-3814; SCH 420814; MK3814
ProtocolIn VitroPreladenant also completely antagonizes cAMP in cells expressing the recombinant human A2A receptor. Preladenant is determined to has KB values of 1.3 nM at the A2A receptor; the value is in good agreement with the Ki value determined in the radioligand binding assay. A similar functional assay with A2B receptor-expressing cells is used to demonstrate selectivity over A2B receptors. In this assay, the KB value for Preladenant is 1.2 μM, indicating that Preladenant is 923-fold selective for the A2A receptor over the A2B receptor
In VivoPreladenant (1 mg/kg) inhibits L-Dopa-induced behavioral sensitization after repeated daily administration, which suggests a reduced risk of the development of dyskinesias. Preladenant exhibits antidepressant-like profiles in models of behavioral despair, namely the mouse tail suspension test and the mouse and rat forced swim test
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
1mM1.9858 mL9.9291 mL19.8582 mL39.7164 mL
5mM0.3972 mL1.9858 mL3.9716 mL7.9433 mL
10mM0.1986 mL0.9929 mL1.9858 mL3.9716 mL
20mM0.0993 mL0.4965 mL0.9929 mL1.9858 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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Concentration
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

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

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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.