- Lu AF21934
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- $32.00 / 1mg
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2024-11-19
- CAS:1445605-23-1
- Min. Order:
- Purity: 97.96%
- Supply Ability: 10g
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| | Lu AF21934 Basic information |
| Product Name: | Lu AF21934 | | Synonyms: | Lu AF21934;CS-2215;LU AF-21934;LU AF 21934;LU-AF21934;LU-AF-21934;2-PYRIMIDINAMINE,4-METHYL-N-[5-METHYL-4-(1H-PYRAZOL-4-YL)-2-THIAZOLYL]-, >98%;LuAF21934, >98%;LU-AF 21934;LU AF 21934;(1S,2R)-N1-(3,4-Dichlorophenyl)-1,2-cyclohexanedicarboxamide;1,2-Cyclohexanedicarboxamide, N1-(3,4-dichlorophenyl)-, (1S,2R)- | | CAS: | 1445605-23-1 | | MF: | C14H16Cl2N2O2 | | MW: | 315.2 | | EINECS: | | | Product Categories: | | | Mol File: | 1445605-23-1.mol |  |
| | Lu AF21934 Chemical Properties |
| Boiling point | 577.6±50.0 °C(Predicted) | | density | 1.386±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | ≥31.5 mg/mL in DMSO; insoluble in H2O; ≥5.03 mg/mL in EtOH with ultrasonic | | form | solid | | pka | 13.23±0.70(Predicted) | | color | White to off-white |
| | Lu AF21934 Usage And Synthesis |
| Biological Activity | ec50: 500 nmlu 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]. | | target | | mGlu4 Receptor 500 nM (EC 50 ) | | | references | [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. |
| | Lu AF21934 Preparation Products And Raw materials |
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