Zonampanel

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

Zonampanel (YM 872) 是一种选择性、有效、高度水溶性、竞争性 AMPA 受体 (AMPAR) 拮抗剂，Ki 为 96 nM。

Zonampanel (YM 872) is a selective, potent and highly water-soluble, competitive AMPA receptor (AMPAR) antagonist with Ki of 96 nM; shows very low affinity for other ionotropic glutamate receptors; competitively antagonizes kainate-induced currents in Xenopus laevis oocytes with a pA2 value of 6.97; exhibits great potential for treatment of neurodegenerative disorders such as stroke.Stroke Discontinued.

Zonampanel inhibits the human MRP4-mediated transport of [3H]oestradiol 17-D-glucuronide in a concentration-dependent manner. In contrast, Zonampanel (up to 1000 mM) does not inhibit the human MRP2- or BCRP-mediated transport of [3H]oestradiol 17-D-glucuronide or [3H]methotrexate. Zonampanel inhibits the uptake of typical substrates by Oat1, Oat2, and Oat3 with inhibition constant (Ki) values of 7.02 to 10.4 μM. A time- and saturable concentration-dependent increase in [14C]Zonampanel uptake is observed in these cells [Km values: 13.4 to 53.6 μM].

In in vivo experiments, probenecid and cimetidine decrease intrinsic clearance for both the renal secretion and biliary excretion of Zonampanel.

YM 872

Membrane Transporter/Ion Channel

iGluR

iGluR

Neurological Disease

Stroke

210245-80-0

331.241

C13H9N5O6

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (150.95 mM)

O=C(O)CN1C(C(NC2=C1C=C(N3C=CN=C3)C([N+]([O-])=O)=C2)=O)=O

7-(1H-Imidazol-1-yl)-6-nitro-2,3-dioxo-3,4-dihydro-1(2H)-quinoxalineacetic acid

(-20℃)

With Ice Pack

≥ 2 years