1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. Lu AF21934

Lu AF21934 

Cat. No.: HY-100366 Purity: 99.27%
Handling Instructions

Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mGlu4 receptor.

For research use only. We do not sell to patients.

Lu AF21934 Chemical Structure

Lu AF21934 Chemical Structure

CAS No. : 1445605-23-1

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1  mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
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10 mg USD 144 In-stock
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25 mg USD 312 In-stock
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50 mg USD 528 In-stock
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100 mg USD 900 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mGlu4 receptor[1].

IC50 & Target[1]

mGlu4 Receptor

500 nM (EC50)

In Vivo

Lu AF21934 treatment shows 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 the basal locomotor activity of mice that are not habituated to activity cages[1]. Lu AF21934 (0.5-5 mg/kg sc) does not influence tremor but at doses of 0.5 and 2.5 mg/kg reverses harmaline-induced hyperactivity. Lu AF21934 at a dose of 2.5 mg/kg potentiates the inhibitory influence of harmaline on the exploratory activity and AP1 during the first 30 min of the measurement and counteracts the harmaline-increased basic activity during the period of 30-90 min[2]. Lu AF21934 (0.1-5 mg/kg) dose-dependently inhibits hyperactivity induced by MK-801 or amphetamine. It also antagonizes head twitches and increases frequency of spontaneous excitatory postsynaptic currents in brain slices, induced by DOI[3].

Molecular Weight

315.20

Formula

C₁₄H₁₆Cl₂N₂O₂

CAS No.

1445605-23-1

SMILES

O=C([[email protected]@H]1[[email protected]](C(N)=O)CCCC1)NC2=CC=C(Cl)C(Cl)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 80 mg/mL (253.81 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1726 mL 15.8629 mL 31.7259 mL
5 mM 0.6345 mL 3.1726 mL 6.3452 mL
10 mM 0.3173 mL 1.5863 mL 3.1726 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Rats: Lu AF21934 is dispersed in 20% (2-hydropropyl)-b-cyclodextrin and are administered subcutaneously (s.c.) 60 min before the test. Lu AF21934 (2, 5, 10 and 15 mg/kg, s.c.) and diazepam (5 mg/kg, i.p.) are administered acutely 1 h before the Vogel’s conflict test. The effects of each drug in all experiments are measured in groups of 8-10 animals[1].

Mice: Lu AF21934 is dispersed in 20% (2-hydropropyl)-b-cyclodextrin and are administered subcutaneously (s.c.) 60 min before the test. Mice are gently placed into the box and allowed to explore for 15 s. Then, each time a mouse passed from one plate to another, the experimenter electrifies the whole floor thus evoking a visible flight reaction of the animal. If the animal continues running, no new shock is delivered for the following 3 s[1].

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

References
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Keywords:

Lu AF21934Lu AF 21934Lu AF-21934mGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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