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首页-小分子抑制剂&激动剂-GPCR-mGluR-JNJ-16259685
JNJ-16259685

Chemical Structure : JNJ-16259685

CAS No.: 409345-29-5

JNJ-16259685 (JNJ16259685)

货号: PC-42138Not For Human Use, Lab Use Only.

JNJ-16259685 (JNJ16259685) is a highly potent, selective, non-competitive and centrally active mGluR1 antagonist with Ki of 0.34 nM.

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10 mg ¥1380 In stock
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50 mg ¥3980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

JNJ-16259685 (JNJ16259685) is a highly potent, selective, non-competitive and centrally active mGluR1 antagonist with Ki of 0.34 nM.
JNJ-16259685 shows no agonist, antagonist or PAM activity toward rat mGlu2/3/4/6 receptors (IC50>10 uM) and does not bind to AMPA, NMDA receptor and other neurotransmitter receptors.
JNJ-16259685 inhibits glutamate-induced Ca2+ mobilization for rat and human mGluR1 with IC50 of 3.24 and 1.21 nM, inhibits glutamate-mediated inositol phosphate production with IC50 of 1.73 nM.
JNJ-16259685 attenuates drug context-induced reinstatement of cocaine seeking in rats.

物理化学性质&存储条件

分子量 325.4015
分子式 C20H23NO3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Methanone, (3,4-dihydro-2H-pyrano[2,3-b]quinolin-7-yl)(cis-4-methoxycyclohexyl)-

参考文献

1. Lavreysen H, et al. Neuropharmacology. 2004 Dec;47(7):961-72.

2. Mabire D, et al. J Med Chem. 2005 Mar 24;48(6):2134-53.

3. Xie X, et al. Psychopharmacology (Berl). 2010 Jan;208(1):1-11.

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