JNJ-39393406

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JNJ-39393406 是一种有效的选择性正变构 α7 nAChR 调节剂，可增强 GH4C1 细胞中表达的人 α7 通道介导的 100 μM 胆碱诱导的细胞内钙升高，EC50 为 660 nM。

JNJ-39393406 is a potent, selective positive allosteric α7 nAChR modulator, potentiates a 100 μM choline-induced rise in intracellular calcium mediated by human α7 channels expressed in GH4C1 cells with EC50 of 660 nM; does not act on α4β2, α3β4 or 5-HT3A channels, as well as α4β2, α3β4 or 5 HT3A channels, and it does not interacts with a panel of 62 receptors and enzymes; shows bell-shaped dose-response activity in the auditory evoked potential (AEP) in DBA2 mice (0.63–5 mg/kg s.c., lower and higher doses were inactive), and model for sensory gating and the attentional set-shifting in rats.Depression Phase 2 Clinical.

——

——

JNJ39393406

Membrane Transporter/Ion Channel

nAChR

nAChR

Neurological Disease

Depression

953428-73-4

416.389

C19H18F2N6O3

>98% (HPLC)

——

O=C(N(C)C)CCN1N=C(NC2=CC=C(OC(F)(F)O3)C3=C2)N=C1C4=CC=NC=C4

1H-1,2,4-Triazole-1-propanamide, 3-[(2,2-difluoro-1,3-benzodioxol-5-yl)amino]-N,N-dimethyl-5-(4-pyridinyl)-

(-20℃)

With Ice Pack

≥ 2 years