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CAS No.: 1363281-27-9

JNJ-46778212 Catalog No. CSN22437

Synonyms: VU 0409551

JNJ-46778212 is an mGlu5 positive allosteric modulator with an EC50 of 260 nM.

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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 mGlu_1–4,6–8 at 10μM. JNJ-46778212 showed excelled central nervous system penetration with K_ps 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]
参考文献

[1] Conde-Ceide S, Martínez-Viturro CM, Alcázar J, Garcia-Barrantes PM, Lavreysen H, Mackie C, Vinson PN, Rook JM, Bridges TM, Daniels JS, Megens A, Langlois X, Drinkenburg WH, Ahnaou A, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Bartolomé-Nebreda JM, Lindsley CW. Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia. ACS Med Chem Lett. 2015 May 20;6(6):716-20. doi: 10.1021/acsmedchemlett.5b00181

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8380 mL
- 14.1900 mL
- 28.3801 mL
- 5 mM
- 0.5676 mL
- 2.8380 mL
- 5.6760 mL
- 10 mM
- 0.2838 mL
- 1.4190 mL
- 2.8380 mL

技术信息

CAS号

1363281-27-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H17FN2O3

运输

蓝冰

分子量

352.36

别名

VU 0409551

溶解度

DMSO	103.0 mg/mL (292.3 mM)
Water	insoluble

动物实验配方

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