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Purity: ≥98%
Lu AF21934 is a novel, potent, selective and brain-penetrant positive allosteric modulator of mGlu4 receptors with an IC50 of 500 nM for human mGlu4. In rats, Lu AF21934 lessens harmaline-induced hyperactivity but not tremor. Lu AF21934's effects are 5-HT1A receptor-dependent. The development of novel antipsychotic medications that are effective against positive, negative, and cognitive symptoms may be facilitated by activation of the mGlu4 receptor.
| Targets |
mGlu4 Receptor ( EC50 = 7500 nM )
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| ln Vivo |
Lu AF21934 treatment shows a dose-dependent anxiolytic-like effect in the stress-induced hyperthermia, four-plate, and marble-burying tests. Flumazenil (10 mg/kg), a benzodiazepine receptor antagonist, inhibits Lu AF21934's (5 mg/kg) anti-hyperthermic effect in the SIH test. This effect is not serotonin dependent. In the tail suspension test, Lu AF21934 does not have antidepressant-like effects on mice; however, it does reduce the basal locomotor activity of mice that have not become accustomed to activity cages[1]. While Lu AF21934 (0.5–5 mg/kg sc) does not affect tremor, harmaline-induced hyperactivity is reversed at doses of 0.5 and 2.5 mg/kg. At a dose of 2.5 mg/kg, Lu AF21934 amplifies the first 30 minutes of the measurement's inhibitory effect of harmaline on AP1 and exploratory activity, and it offsets the harmaline-induced rise in basic activity over the next 30 to 90 minutes[2]. Hyperactivity brought on by MK-801 or amphetamine is dose-dependently inhibited by Lu AF21934 (0.1–5 mg/kg). It also makes head twitches more aggressive and raises the frequency of DOI-induced spontaneous excitatory postsynaptic currents in brain slices[3].
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| Animal Protocol |
Rats: The 20% (2-hydropropyl)-b-cyclodextrin-dispersed Lu AF21934 is applied subcutaneously (s.c.) 60 minutes prior to the test. Acute administration of Lu AF21934 (2, 5, 10 and 15 mg/kg, s.c.) and diazepam (5 mg/kg, i.p.) occurs one hour prior to the Vogel's conflict test. In all experiments, groups of eight to ten animals are used to measure the effects of each drug[1].
Mice: Sixty minutes prior to the test, Lu AF21934 is applied subcutaneously (s.c.) after being diluted in 20% (2-hydropropyl)-b-cyclodextrin. The mice are inserted carefully into the box and given fifteen seconds to explore. Once the mouse has moved from one plate to another, the experimenter electrifies the entire floor, causing the mouse to visibly flee. No more shocks are given for the next three seconds if the animal keeps running[1]. |
| References |
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| Molecular Formula |
C14H16CL2N2O2
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|---|---|
| Molecular Weight |
315.1950
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| Exact Mass |
314.06
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| Elemental Analysis |
C, 53.35; H, 5.12; Cl, 22.49; N, 8.89; O, 10.15
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| CAS # |
1445605-23-1
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| Appearance |
Solid powder
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| SMILES |
C1CC[C@@H]([C@@H](C1)C(=O)N)C(=O)NC2=CC(=C(C=C2)Cl)Cl
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| InChi Key |
AVKZWCJNDWOBAM-ZJUUUORDSA-N
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| InChi Code |
InChI=1S/C14H16Cl2N2O2/c15-11-6-5-8(7-12(11)16)18-14(20)10-4-2-1-3-9(10)13(17)19/h5-7,9-10H,1-4H2,(H2,17,19)(H,18,20)/t9-,10+/m1/s1
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| Chemical Name |
(1R,2S)-2-N-(3,4-dichlorophenyl)cyclohexane-1,2-dicarboxamide
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| Synonyms |
Lu-AF21934; Lu-AF-21934; Lu-AF 21934; Lu AF21934; Lu AF-21934; Lu AF 21934; LuAF21934; LuAF-21934; LuAF 21934
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 80 mg/mL (~253.8 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.93 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
 Effect of Lu AF21934 (A) and Lu AF32615 (B) on the locomotor activity of mice habituated to activity cages.Br J Pharmacol.2013 Aug;169(8):1824-39. |
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 The suppression of DOI-induced head twitches by Lu AF21934 (A) and reference compound clozapine (B) in wild type (WT) and mGlu4−/−(KO) mice.Br J Pharmacol.2013 Aug;169(8):1824-39. |
 Suppression by Lu AF21934 (A) or Lu AF32615 (B) of the increase in sEPSCs activity induced by DOI recording after 10 min incubation with DOI and after 10 min incubation with Lu AF21934 or Lu AF32615 in the continuous presence of DOI. *P< 0.05 versus DOI effect; pairedt-test.Br J Pharmacol.2013 Aug;169(8):1824-39. |
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