ETHYL-L-NIO (HYDROCHLORIDE) Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMF: 0.3 mg/ml; DMSO: 2 mg/ml; Ethanol: 2.5 mg/ml; PBS (pH 7.2): 5 mg/ml

form 

A crystalline solid

ETHYL-L-NIO (HYDROCHLORIDE) Usage And Synthesis

Description

Ethyl-L-NIO, the saturated analog of vinyl-L-NIO, is a modestly selective NOS inhibitor. The K_i values for inhibition of nNOS, eNOS, and iNOS by ethyl-L-NIO are 5.3, 18, and 12 μM, respectively, as determined using initial rate measurements. However when evaluating the K_i/K_m ratio, ethyl-L-NIO does not show biologically significant selectivity for nNOS over eNOS, and instead favors iNOS (K_i/K_m = 3.79, 5, and 0.96 μM, respectively). Although ethyl-L-NIO inhibits nNOS, it does not inactivate nNOS in the presence of NADPH and O₂.

Uses

Ethyl-L-NIO hydrochloride is a potent and competitive human dimethylarginine dimethylaminohydrolase 1 (hDDAH-1) inhibitor with an IC50 of 70 μM and a Ki of 32 μM[1].

References

[1] Kotthaus J, et al. Structure-activity relationship of novel and known inhibitors of human dimethylarginine dimethylaminohydrolase-1: alkenyl-amidines as new leads. Bioorg Med Chem. 2008 Dec 15;16(24):10205-9. DOI:10.1016/j.bmc.2008.10.058

ETHYL-L-NIO (HYDROCHLORIDE)(150403-97-7)Related Product Information

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