Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
H4430 |
WAY-213613 |
868359-05-1 | WAY-213613 (WAY213613) is a potent, non-substrate inhibitor of EAAT2 (GLT-1) with IC50 of 85 nM, displays > 44-fold selectivity over EAAT1 and EAAT3; also exhibits no activity towards ionotropic and metabotropic glutamate receptors. |
H4429 |
V-9302 |
1855871-76-9 |
V-9302 (V9302) is a competitive, selective antagonist of transmembrane glutamine flux that selectively and potently targets the amino acid transporter ASCT2 with IC50 of 9.6 uM; displays 100-fold improvement in potency over γ-L-glutamyl-p-nitroanilide (GPNA); attenuates cancer cell growth and proliferation (CRC cell lines EC50=9-15 uM), increases cell death, and increases oxidative stress, which collectively contribute to antitumor responses in vitro and in vivo. |
H4428 |
UCPH-102 |
1229591-56-3 |
UCPH-102 is a selective, brain penetrant inhibitor of EAAT1 (Excitatory amino acid transporter 1) with IC50 of 420 nM; exhibits no inhibitory activity aganist EAAT2-5 (>300 uM); has been shown to cross the blood-brain barrier, and become a valuable tool for studying the role of EAAT1 in brain. |
H4427 |
UCPH-101 |
1118460-77-7 |
UCPH-101 is a selective non-substrate inhibitor of EAAT1 (Excitatory amino acid transporter 1) with IC50 of 660 nM; dispalys >50-fold selectivity over EAAT2 and EAAT3, and has no significant inhibition at EAAT4 or EAAT5. |
H4426 |
Trigriluzole |
1926203-09-9 | 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. |
H4425 |
NBI-59159 |
1026096-83-2 | NBI-59159 (NBI59159) is a potent EAAT3-preferring inhibitor. |
H4424 |
LDN 0212320 |
894002-50-7 |
LDN0212320 (OSU 0212320) is a small-molecule activator of glutamate transporter EAAT2 translation with EC50 of 1.83 uM; activates PKC and subsequent Y-box-binding protein 1 (YB-1), which regulates activation of EAAT2 translation; protects cultured neurons from glutamate-mediated excitotoxic injury and death via EAAT2 activation in a murine model; markedly delays motor function decline and extends lifespan in an animal model of ALS, reduces mortality, neuronal death, and spontaneous recurrent seizures in a pilocarpine-induced temporal lobe epilepsy model. |
H4423 |
L-g-glutamyl-p-nitroanilide hydrochloride |
67953-08-6 |
L-g-glutamyl-p-nitroanilide hydrochloride is a potent, competitive inhibitor of the neutral amino acid transporter ASCT2 (SLC1A5) with pKa of 13.79. |
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