JNJ-46778212
产品说明书
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同义名 : | VU 0409551 |
| CAS号 : | 1363281-27-9 | |
| 货号 : | A693152 | |
| 分子式 : | C20H17FN2O3 | |
| 纯度 : | 99% | |
| 分子量 : | 352.359 | |
| MDL号 : | MFCD29047143 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(297.99 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | The metabotropic glutamate receptor subtype 5 (mGlu5) is a G protein-coupled receptor implicated in schizophrenia. JNJ-46778212 is a mGlu5 positive allosteric modulator with an EC50 value of 260nM and with 84% Glu Max. It is highly selective for mGlu5 relative to mGlu1–4,6–8 at 10μM. JNJ-46778212 showed excelled central nervous system penetration with Kps of 1.0 and 2.3 for mouse and rat, respectively. It was inactive in the hERG patch clamp (22% inhibition at 3μM) and was clean in a CV-relevant ion channel panel (hERG, Ca, Na channels, IC50s >10μM). JNJ-46778212 exhibited robust dose-responsive efficacy with a maximum reversal of ∼78% at 100mg/kg (p.o.) and a minimum effective dose of 10mg/kg (p.o.) with an ED50 value of 23mg/kg in a preclinical assay. In an investigational new drug-enabling study, chronic administration of JNJ-46778212 at a dose of 360mg/kg (p.o.) for 30 days induced neuronal death (indicated by Fluoro-Jade C staining) in rats.[1] | ||
| 作用机制 | JNJ-46778212 is a potent, selective, and orally bioavailable positive allosteric modulator of mGlu5.[1] | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.84mL 0.57mL 0.28mL |
14.19mL 2.84mL 1.42mL |
28.38mL 5.68mL 2.84mL |
| 参考文献 |
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