1598424-76-0

1598424-76-0 structure

Name: BMS-466442
Chemical Name: Methyl 1-benzyl-N-{[6-(benzyloxy)-5-methoxy-1H-indol-2-yl]carbonyl}-L-histidinate
CAS Number: 1598424-76-0
Molecular Formula: C₃₁H₃₀N₄O₅
Molecular Weight: 538.594
Catalog: Signaling Pathways GPCR/G Protein Adrenergic Receptor
Create Date: 2018-06-12 14:07:30
Modify Date: 2024-01-10 18:18:43
BMS-466442 is a potent and selective inhibitor of asc-1 (alanine serine cysteine transporter-1), with an IC50 of 11 nM. BMS-466442 inhibits [3H] D-serine uptake into rat brain synaptosomes, with an IC50 of 400 nM. BMS-466442 can be used for schizophrenia research[1][2].

Name	Methyl 1-benzyl-N-{[6-(benzyloxy)-5-methoxy-1H-indol-2-yl]carbonyl}-L-histidinate
Synonyms	L-Histidine, N-[[5-methoxy-6-(phenylmethoxy)-1H-indol-2-yl]carbonyl]-1-(phenylmethyl)-, methyl ester Methyl 1-benzyl-N-{[6-(benzyloxy)-5-methoxy-1H-indol-2-yl]carbonyl}-L-histidinate

Description	BMS-466442 is a potent and selective inhibitor of asc-1 (alanine serine cysteine transporter-1), with an IC50 of 11 nM. BMS-466442 inhibits [3H] D-serine uptake into rat brain synaptosomes, with an IC50 of 400 nM. BMS-466442 can be used for schizophrenia research[1][2].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Transporter Research Areas >> Neurological Disease
Target	IC50: 1 nM (asc-1), 420 nM (dopamine transporter), 6.1 μM (Adrenergic α1D receptor), ≥10 μM (LAT-2), ≥10 μM (ASCT-2)[1]
In Vitro	BMS-466442 dose-dependently inhibits asc-1 activity in human asc-1 expressing cells and primary cultures with IC50 values of 36.8 ± 11.6 nM and 19.7 ± 6.7 nM, respectively[1].
References	[1]. Brown JM, et al. In vitro Characterization of a small molecule inhibitor of the alanine serine cysteine transporter -1 (SLC7A10). J Neurochem. 2014 Apr;129(2):275-83. [2]. Torrecillas IR, et al. Inhibition of the Alanine-Serine-Cysteine-1 Transporter by BMS-466442. ACS Chem Neurosci. 2019 May 15;10(5):2510-2517.