Lu AF21934 |
| Katalog-Nr.GC15992 |
Lu AF21934 ist ein selektiver und ins Gehirn eindringender positiver allosterischer Modulator des mGlu4-Rezeptors mit einem EC50-Wert von 500 nM fÜr den mGlu4-Rezeptor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1445605-23-1
Sample solution is provided at 25 µL, 10mM.
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EC50: 500 nM
Lu AF21934 is a positive allosteric modulator of mGlu4 receptors.
The mGlu4 receptor subtype of the group III mGlu is mainly a presynaptic auto- or hetero-receptor. Its stimulation results in an inhibition of glutamatergic or GABAergic transmission and release
In vitro: Lu AF21934 has been identified as a brain-penetrating positive allosteric modulator of mGlu4 receptors. In broad in-vitro screens, Lu AF21934 could potentiate the glutamate response at the mGlu4 receptor with an Emax=120% and a glutamate fold-shift FS=5. Lu AF21934 did not showed any significant affinity for 70 GPCRs at 10 μM, but acted as a weak positive allosteric modulator of mGlu6 receptor, as well as an antagonist of adenosine A2A and 5-HT2B receptors [1].
In vivo: In rats, harmaline triggered tremor as manifested by an increase in the power within 9-15Hz band and in the tremor index. Harmaline also induced a biphasic effect on mobility, initially inhibiting the exploratory locomotor activity of rats, followed by an increase in their basic activity. Lu AF21934 at 0.5-5 mg/kg sc did not influence tremor but at doses of 0.5 and 2.5 mg/kg reversed harmaline-induced hyperactivity. MGlu4 mRNA expression was found to be high in the cerebellar cortex and low in the inferior olive [1].
Clinical trial: Up to now, Lu AF21934 is still in the preclinical development stage.
Reference:
[1] Ossowska K,Wardas J,Berghauzen-Maciejewska K,et al. Lu AF21934, a positive allosteric modulator of mGlu4 receptors, reduces the harmaline-induced hyperactivity but not tremor in rats. Neuropharmacology.2014 Aug;83:28-35.
Animal experiment: | 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]. |
References: [1]. Sławińska A, et al. Anxiolytic- but not antidepressant-like activity of Lu AF21934, a novel, selective positive allosteric modulator of the mGlu₄ receptor. Neuropharmacology. 2013 Mar;66:225-35. | |
| Cas No. | 1445605-23-1 | SDF | |
| Chemical Name | (1R,2S)-2-((3,4-dichlorophenyl)carbamoyl)cyclohexanecarbimidic acid | ||
| Canonical SMILES | ClC1=C(C=C(C=C1)NC([C@]2(CCCC[C@]2(C(O)=N)[H])[H])=O)Cl | ||
| Formula | C14H16Cl2N2O2 | M.Wt | 315.2 |
| Löslichkeit | ≥ 31.5mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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