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Trigriluzole

Cat. No. M40547
Trigriluzole Structure
Synonym:

Troriluzole; BHV-4157

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Biological Activity

Trigriluzole is an excitatory amino acid transporter protein 2 (EAAT2) modulator that increases the uptake of glutamate at neuronal synapses by increasing the expression and enhancing the function of EAAT in glial cells, thereby decreasing glutamate levels in neuronal synapses. It can be used in studies related to spinocerebellar ataxia (SCA) and anxiety disorders.

Chemical Information
Molecular Weight 419.38
Formula C15H16F3N5O4S
CAS Number 1926203-09-9
Solubility (25°C) DMSO 50 mg/mL
Storage -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ann W Silk et al. Eur J Med Res. A phase Ib dose-escalation study of troriluzole (BHV-4157), an oral glutamatergic signaling modulator, in combination with nivolumab in patients with advanced solid tumors

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Troriluzole Hydrochloride is the hydrochloride form of Troriluzole, and is also an excitatory amino acid transporter protein 2 (EAAT2) modulator, which increases glutamate uptake at neuronal synapses by increasing the expression of EAAT in neuroglia and enhancing its function, thereby decreasing glutamate levels in neuronal synapses. It can be used in studies related to spinocerebellar ataxia (SCA) and anxiety disorders.

TFB-TBOA

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  Catalog
Abmole Inhibitor Catalog




Keywords: Trigriluzole, Troriluzole; BHV-4157 supplier, EAAT, inhibitors, activators


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