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Chemical Structure : JNJ-61432059
CAS No.: 2035814-59-4
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $288 | In stock | |
| 10 mg | $478 | In stock | |
| 25 mg | Get quote | ||
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 344.35 | |
| Formula | C20H13FN4O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
5-(2-(4-fluorophenyl)pyrazolo[1,5-c]pyrimidin-3-yl)indolin-2-one |
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1. Savall BM, et al. ACS Med Chem Lett. 2018 Dec 26;10(3):267-272.
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