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| N-(5-CHLORO-2,4-DIMETHOXYPHENYL)-N'-(5-METHYL-3-ISOXAZOLYL)-UREA Basic information |
| Product Name: | N-(5-CHLORO-2,4-DIMETHOXYPHENYL)-N'-(5-METHYL-3-ISOXAZOLYL)-UREA | | Synonyms: | PNU 120596;N-(5-CHLORO-2,4-DIMETHOXYPHENYL)-N'-(5-METHYL-3-ISOXAZOLYL)-UREA;N-(5-Chloro-2,4-dimethoxphenyl)-N'-(5-methyl-3-isoxazolyl)-urea;1-(5-Chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea;Nsc 216666;Urea, N-(5-chloro-2,4-dimethoxyphenyl)-N'-(5-methyl-3-isoxazolyl)-;PNU-120596;PNU120596; NSC 216666;CS-224 | | CAS: | 501925-31-1 | | MF: | C13H14ClN3O4 | | MW: | 311.72 | | EINECS: | | Product Categories: | Inhibitors | | Mol File: | 501925-31-1.mol |
| N-(5-CHLORO-2,4-DIMETHOXYPHENYL)-N'-(5-METHYL-3-ISOXAZOLYL)-UREA Chemical Properties |
| density | 1.403 | | storage temp. | room temp | | solubility | DMSO: >10mg/mL | | form | White solid | | color | white to off-white |
| N-(5-CHLORO-2,4-DIMETHOXYPHENYL)-N'-(5-METHYL-3-ISOXAZOLYL)-UREA Usage And Synthesis |
| Uses | PNU 120596 is a type II positive allosteric modulator. | | Biological Activity | Positive allosteric modulator of α 7 neuronal nicotinic acetylcholine receptors (EC 50 = 216 nM), with no detectable effect on α 4 β 2, α 3 β 4 and α 9 α 10 receptors. Active in vivo following systemic administration. | | Biochem/physiol Actions | An allosteric modulator of α7 nicotinic receptors, N-(5-chloro-2,4-dimethoxyphenyl)-N′-(5-methyl-3-isoxazolyl)-urea (PNU-120596), causes conformational changes in the extracellular ligand binding domain similar to those caused by acetylcholinePNU-120596 is a positive allosteric modulator selective for the α7 nicotinic acetylcholine receptor. PNU-120596 produces no detectable change in currents mediated by α4β2, α3β4, α9α10 nAChRs. It increases channel mean open time, but does not affect ion selectivity. It does not bind at the agonist binding site, but induces conformational changes similar to the natural effector. | | references | [1] hurst r s, hajós m, raggenbass m, et al. a novel positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. the journal of neuroscience, 2005, 25(17): 4396-4405.[2] bertrand d, gopalakrishnan m. allosteric modulation of nicotinic acetylcholine receptors. biochemical pharmacology, 2007, 74(8): 1155-1163. |
| N-(5-CHLORO-2,4-DIMETHOXYPHENYL)-N'-(5-METHYL-3-ISOXAZOLYL)-UREA Preparation Products And Raw materials |
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