DL-Threo-β-Benzyloxyaspartic acid (DL-TBOA) is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO ≥ 100 mg/mL|
 Elena Pedraz-Cuesta, et al. BMC Cancer. The glutamate transport inhibitor DL-Threo-β-Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells
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WAY-213613 hydrochloride is a potent, selective nonsubstrate reuptake inhibitor of GLT-1/EAAT2 with IC50 of 85 nM EAAT2.
Way-213613 is a potent, selective, non-substrate reuptake inhibitor of GLT-1/EAAT2 with an IC50 of 85 nM against EAAT2. The selectivity of WAY-213613 hydrochloride to EAAT1 and EAAT3 was 59 and 44 times higher (IC50 was 5 and 3.8 μM, respectively). Way-213613 has no activity on ionic and metabolic glutamate receptors.
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