BMS-466442

Names

[ Name ]:
BMS-466442

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
827.3±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₃₁H₃₀N₄O₅

[ Molecular Weight ]:
538.594

[ Flash Point ]:
454.1±34.3 °C

[ Exact Mass ]:
538.221619

[ LogP ]:
4.33

[ Vapour Pressure ]:
0.0±3.0 mmHg at 25°C

[ Index of Refraction ]:
1.630

Related Compounds

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