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Lu AF21934

Lu AF21934
Lu AF21934 is a brain-penetrant and selective mGlu4 receptor positive allosteric modulator (IC50: 500 nM, human).
Catalog No. T3539Cas No. 1445605-23-1
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Purity:97.96%
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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).
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.
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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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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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
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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