Trigriluzole

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

Trigriluzole (BHV-4157) 是一种新型谷氨酸调节剂，用于治疗轻中度阿尔茨海默病 (AD)； Trigriluzole 是第三代前药和调节谷氨酸的新化学实体。

Trigriluzole (BHV-4157) is a novel glutamate modulator for the treatment of mild-to-moderate Alzheimer’s disease (AD); Trigriluzole is a third-generation prodrug and new chemical entity that modulates glutamate, the most abundant excitatory neurotransmitter in the human body. Trigriluzole has a wide range of pharmacological actions, including interactions with several types of ion channels, cellular signaling mechanisms and facilitation of glutamate reuptake. Some potential targets related to trigriluzole’s mechanism of action include (1) reducing presynaptic glutamate release through actions at the voltage-gated ion channels, (2) facilitating glutamate uptake via EAATs located on glial cells, (3) enhancing transmission through synaptic AMPA receptors, (4) altering GABAergic neurotransmission, and (5) effecting neurotrophic agents such as BDNF.Anxiety Phase 3 Clinical.

Troriluzole is absorbed systemically and cleaves into riluzole by aminopeptidases.

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BHV-4157 | BHV4157

Membrane Transporter/Ion Channel

Glutamate Transporter

Glutamate Transporter

Neurological Disease

Anxiety

1926203-09-9

419.379

C15H16F3N5O4S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (119.22 mM)

O=C(NC(CNC(CN)=O)=O)CN(C)C1=NC2=CC=C(OC(F)(F)F)C=C2S1

Glycylglycyl-N2-methyl-N1-[6-(trifluoromethoxy)-1,3-benzothiazol-2-yl]glycinamide

(-20℃)

With Ice Pack

≥ 2 years