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Lu AF21934

Catalog No. T3539Cas No. 1445605-23-1

Lu AF21934 is a brain-penetrant and selective mGlu4 receptor positive allosteric modulator (IC50: 500 nM, human).

Lu AF21934

Lu AF21934

Purity: 97.96%
Catalog No. T3539Cas No. 1445605-23-1
Lu AF21934 is a brain-penetrant and selective mGlu4 receptor positive allosteric modulator (IC50: 500 nM, human).
Pack SizePriceAvailabilityQuantity
1 mg$32In Stock
5 mg$72In Stock
10 mg$129In Stock
25 mg$243In Stock
50 mg$388In Stock
100 mg$619In Stock
1 mL x 10 mM (in DMSO)$72In Stock
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Purity:97.96%
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Product Introduction

Bioactivity
Description
Lu AF21934 is a brain-penetrant and selective mGlu4 receptor positive allosteric modulator (IC50: 500 nM, human).
Targets&IC50
mGlu4 (human):500 nM
In vivo
Lu AF21934 treatment exhibits a dose-dependent anxiolytic-like effect in the stress-induced hyperthermia, four-plate, and marble-burying tests. The anti-hyperthermic effect of Lu AF21934 (5 mg/kg) in the SIH test is inhibited by the benzodiazepine receptor antagonist flumazenil (10 mg/kg) and is not serotonin-dependent. Lu AF21934 does not produce antidepressant-like effects in the tail suspension test in mice; however, it decreases basal locomotor activity in mice not habituated to activity cages.
Kinase Assay
The receptor-expressing CHO cells are seeded into 24-well plates at a density of 4×104 cells/well and cultured for 1 day. The cells are then incubated with [5,6,8,9,11,12,14,15-3H]arachidonic acid (11 kBq/well) for 1 day and ished with DMEM supplemented with 20 mM HEPES and 0.2% BSA. The cells are then preincubated with the compounds (Sufugolix) at 37 °C for 60 min and the reaction is started by addition of LHRH (1 nM). After incubation at37 °C for 40 min, radioactivity in the medium is measured with a liquid scintillation counter[1].
Chemical Properties
Molecular Weight315.2
FormulaC14H16Cl2N2O2
Cas No.1445605-23-1
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 16.67 mg/mL (52.88 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.1726 mL15.8629 mL31.7259 mL158.6294 mL
5 mM0.6345 mL3.1726 mL6.3452 mL31.7259 mL
10 mM0.3173 mL1.5863 mL3.1726 mL15.8629 mL
20 mM0.1586 mL0.7931 mL1.5863 mL7.9315 mL
50 mM0.0635 mL0.3173 mL0.6345 mL3.1726 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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