D,L-Buthionine-(S,R)-sulfoximine (Butionine sulfoximine)

A γ-glutamylcysteine synthetase inhibitor

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50mg

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Background

D,L-Buthionine-(S,R)-sulfoximine is an inhibitor of γ-glutamylcysteine synthetase that induces 100% inhibition at a concentration of 10 μM in an enzyme assay.¹ It is selective for γ-glutamylcysteine synthetase, lacking activity at glutamine synthetase at concentrations up to 500 μM. D,L-Buthionine-(S,R)-sulfoximine (32 mmol/kg, i.p.) reduces renal glutathione in mice without inducing abnormal behavior or convulsions. It has antiparasitic activity, eliminating T. brucei from the bloodstream of infected mice via depletion of intratrypanosomal glutathione and induction of oxidative stress at a dose of 4 mmol/kg.² D,L-Buthionine-(S,R)-sulfoximine is an isomeric mixture of L-buthionine-S-sulfoxime, L-buthionine-R-sulfoxime, D-buthionine-S-sulfoxime, and D-buthionine-R-sulfoxime.

1.Griffith, O.W., and Meister, A.Potent and specific inhibition of glutathione synthesis by buthionine sulfoximine (S-n-butyl homocysteine sulfoximine)J. Biol. Chem.254(16)7558-7560(1979) 2.Arrick, B.A., Griffith, O.W., and Cerami, A.Inhibition of glutathione synthesis as a chemotherapeutic strategy for trypanosomiasisJ. Exp. Med.153(3)720-725(1981)

Protocol

Animal experiment:

Mice[2]D,L-Buthionine-(S,R)-sulfoximine is dissolved in sterile 0.9% saline, filtered through a 0.2-p.m polysulfone membrane filter, and administered by 48-h continuous iv. infusion at a dose of 300 mg/kg/day and 600 mg/kg/day starting at 24 h before doxorubicin administration. In vivo GSH levels after treatment with D,L-Buthionine-(S,R)-sulfoximine at a dose of 300 mg/kg and 600 mg/kg for 24 h as an iv. continuous infusion in munine plasma and in tumor tissue of HT1080 and HT1080/DR4 xenografts is measured[2].

参考文献:

[1]. Griffith OW, et al. Potent and specific inhibition of glutathione synthesis by buthionine sulfoximine (S-n-butyl homocysteine sulfoximine). J Biol Chem. 1979 Aug 25;254(16):7558-60.
[2]. Vanhoefer U, et al. d,l-buthionine-(S,R)-sulfoximine potentiates in vivo the therapeutic efficacy of doxorubicin against multidrug resistance protein-expressing tumors. Clin Cancer Res. 1996 Dec;2(12):1961-8.