VU 0361737

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

VU 0361737 是 mGlu4 受体的特异性正变构调节剂 (PAM)。VU 0361737 对于人类受体的 EC50 为 240 nM。

VU 0361737 is a selective positive allosteric modulator at mGluR-4 (EC50 values are 240 and 110 nM at human and rat receptors respectively).

VU0361737 displays weak activity at mGlu5 and mGlu8 receptors and inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors.VU0361737 (1-10 μM) partially attenuates the Staurosporine (HY-15141)- and Doxorubicin (HY-15142)-evoked cell death on human neuroblastoma SH-SY5Y cells.

VU0361737 exhibits terminal elimination half-lives (rat 1.9 h) due to high plasma clearance (894 mL/min/kg) following Intraperitoneal injection ( rat 10 mg/kg). Animal Model:Male Sprague-Dawley rats (225-250 g)Dosage:10 mg/kg (Pharmacokinetic Analysis)Administration:Intraperitoneal injection Result:T1/2 (1.9 h).

VU 0361737, VU-0361737, VU0361737

Others

Other Targets

mGluR4 (Human)| mGluR4 (Rat )

Neurological Disease

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1161205-04-4

262.69

C13H11ClN2O2

>98% (HPLC)

DMSO : ≥ 43 mg/mL 163.69 mM

COc1c(ccc(c1)NC(=O)c1ccccn1)Cl

N-(4-Chloro-3-methoxyphenyl)-2-pyridinecarboxamide

(-20℃)

With Ice Pack

≥ 2 years