- L-Glutamine
- CPPHA
- VU 0357121
- Dipraglurant
- CTEP (RO4956371)
| Lu AF21934positive allosteric modulator of mGlu4 receptors |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.70%
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Chemical structure
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| Cas No. | 1445605-23-1 | SDF | Download 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 |
| Solubility | ≥31.5mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
