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Submit ReviewLY 487379 hydrochloride
说明： Selective positive allosteric modulator of mGlu2 receptors
化学名： 2,2,2-Trifluoro-N-[4-(2-methoxyphenoxy)phenyl]-N-(3-pyridinylmethyl)ethanesulfonamide hydrochloride
纯度： ≥99% (HPLC)
生物活性 for LY 487379 hydrochloride
LY 487379 hydrochloride is a positive allosteric modulator selective for mGlu2 receptors. Potentiates glutamate-stimulated [35S]GTPγS binding (EC50 values are 1.7 and > 10 μM for mGlu2 and mGlu3 receptors respectively). Devoid of any activity at mGlu5 and mGlu7 receptors. Promotes cognitive flexibility in a rat model.
技术数据 for LY 487379 hydrochloride
| 分子量 | 488.91 |
| 公式 | C21H19F3N2O4S.HCl |
| 储存 | Store at -20°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 353229-59-1 |
| PubChem ID | 56972206 |
| InChI Key | LPWFRDWTOKLHJC-UHFFFAOYSA-N |
| Smiles | O=S(N(CC3=CC=CN=C3)C1=CC=C(OC2=CC=CC=C2OC)C=C1)(CC(F)(F)F)=O.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for LY 487379 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 48.89 | 100 | |
| ethanol | 24.45 | 50 |
制备储备液 for LY 487379 hydrochloride
以下数据基于产品分子量 488.91。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.05 mL | 10.23 mL | 20.45 mL |
| 5 mM | 0.41 mL | 2.05 mL | 4.09 mL |
| 10 mM | 0.2 mL | 1.02 mL | 2.05 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
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产品说明书 for LY 487379 hydrochloride
参考文献 for LY 487379 hydrochloride
参考文献是支持产品生物活性的出版物。
Johnson et al (2003) Discovery of allosteric potentiators for the metabotropic glutamate 2 receptor: synthesis and subtype selectivity of N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,-trifluoroethylsulfonyl)pyrid-3-ylmethyl-amine. J.Med.Chem. 46 3189 PMID: 12852748
Schaffhauser et al (2003) Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2. Mol.Pharmacol. 64 798 PMID: 14500736
Poisik et al (2005) Metabotropic glutamate receptor 2 modulates excitatory synaptic transmission in the rat globus pallidus. Neuropharmacology 49 57 PMID: 15993439
Nikiforuk et al (2010) Effects of a positive allosteric modulator of group II metabotropic glutamate receptors, LY487379, on cognitive flexibility and impulsive-like responding in rats. J.Pharmacol.Exp.Ther. 335 665 PMID: 20739457
If you know of a relevant reference for LY 487379 hydrochloride, please let us know.
关键词: LY 487379 hydrochloride, LY 487379 hydrochloride supplier, Positive, allosteric, modulators, pam, selective, mGlu2, mGluR2, mGlur, Group, II, Receptors, Glutamate, Metabotropic, LY487379, hydrochloride, (Metabotropic), 3283, Tocris Bioscience
4 篇 LY 487379 hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 LY 487379 hydrochloride 的部分引用包括：
Motolese et al (2015) Targeting type-2 metabotropic glutamate receptors to protect vulnerable hippocampal neurons against ischemic damage. Neuropharmacology 8 66 PMID: 26496940
Copeland et al (2015) Neuronal activity patterns in the mediodorsal thalamus and related cognitive circuits are modulated by metabotropic glutamate receptors. Nat Commun 92 16 PMID: 25576798
Yin et al (2014) Selective actions of novel allosteric modulators reveal functional heteromers of metabotropic glutamate receptors in the CNS. J Neurosci 34 79 PMID: 24381270
Scholler (2017) Allosteric nanobodies uncover a role of hippocampal mGlu2 receptor homodimers in contextual fear consolidation. Nat Commun 8 1967 PMID: 29213077
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