JNJ-61432059 | TARPγ-8 AMPAR NAM | Probechem Biochemicals

Chemical Structure : JNJ-61432059

CAS No.: 2035814-50-5

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JNJ-61432059 (JNJ 61432059)

货号: PC-20320Not For Human Use, Lab Use Only.

JNJ-61432059 is a potent, TARPγ-8 selective AMPAR negative modulator with pIC50 of 9.7 in FLIPR assay using HEK-293 cells expressing human GluA1o-γ-8.

规格	价格	库存
5 mg	￥2280	In stock
10 mg	￥3680	In stock
25 mg	￥5580	In stock
50 mg	￥8580	In stock
100 mg		Get quote

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生物&药学活性

JNJ-61432059 is a potent, TARPγ-8 selective AMPAR negative modulator with pIC50 of 9.7 in FLIPR assay using HEK-293 cells expressing human GluA1o-γ-8.
JNJ-61432059 does not inhibit glutamate-induced calcium-flux in heterologous cells that coexpressed AMPARs with any TARP other than γ-8 at 10 uM.
JNJ-61432059 also shows no activity against a panel of 52 receptors, ion channels, and transporters using radioligand displacement assays.
JNJ-61432059 demonstrates robust target engagement observed in vivo, shows protection in the corneal kindling model with ED50 of 1.3 mg/kg.
JNJ-61432059 (5 mg/kg, p.o.) demonstrates anticonvulsant efficacy and seizure protection in corneal kindling and pentylenetetrazole (PTZ) anticonvulsant models.

物理化学性质&存储条件

分子量	443.48
分子式	C25H22FN5O2
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	5-[2-(4-Fluorophenyl)-7-(4-hydroxy-1-piperidinyl)pyrazolo[1,5-c]pyrimidin-3-yl]-1,3-dihydro-2H-indol-2-one

参考文献

1. Savall BM, et al. ACS Med Chem Lett. 2018 Dec 26;10(3):267-272.

JNJ-61432059 (JNJ 61432059)

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JNJ-61432059 (JNJ 61432059)

生物&药学活性

物理化学性质&存储条件

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