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1,4-PBIT(dihydrobromide)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
1,4-PBIT(dihydrobromide)图片
CAS NO:157254-60-9
包装与价格:
包装价格(元)
10mg电议
50mg电议
100mg电议
500mg电议

产品介绍
potent inhibitor of purified human iNOS and nNOS
Cas No.157254-60-9
化学名S,S'-1,4-phenylene-bis(1,2-ethanediyl)bis-isothiourea, dihydrobromide
Canonical SMILESN/C(SCCC1=CC=C(CCS/C(N)=N/[H])C=C1)=N/[H].Br.Br
分子式C12H18N4S2o 2HBr
分子量444.2
溶解度≤20mg/ml in DMSO;20mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

1,4-PBIT (dihydrobromide) is a potent inhibitor of iNOS and nNOS with Ki values of 7.4 and 16 nM, respectively [1].

Nitric oxide (NO) is an endogenously produced inorganic free radical gas which has been implicated in blood pressure homeostasis, platelet aggregation, neurotransmission, and immunological defense mechanisms. NO is synthesized by three isoforms of nitric oxide synthase (NOS): nNOS, eNOS and iNOS [1].

1,4-PBIT, also known as S,S’-(1,4-Phenylenebis(1,2-ethanediyl))bisisothiourea, is a potent and selective iNOS and nNOS inhibitor. 1,4-PBIT inhibited purified human iNOS, eNOS and nNOS with Ki values of 7.4 nM, 360 nM and 16 nM, respectively. In DLD-1 cells, 1,4-PBIT inhibited human iNOS with IC50 value of 30 μM, presumably to poor membrane permeability [1].

In anesthetized rats, 1,4-PBIT (10 mg/kg, given 1 h after LPS administration), 1,4-PBIT effectively reversed the systemic hypotension, reduced the exhaled NO concentration and prevented acute lung injury. 1,4-PBIT also significantly depressed LPS-induced mRNA expressions of iNOS and IL-1β[2].

References:
[1].  Garvey EP, Oplinger JA, Tanoury GJ, et al. Potent and selective inhibition of human nitric oxide synthases. Inhibition by non-amino acid isothioureas. J Biol Chem. 1994 Oct 28;269(43):26669-76.
[2].  Wang D, Wei J, Hsu K, et al. Effects of nitric oxide synthase inhibitors on systemic hypotension, cytokines and inducible nitric oxide synthase expression and lung injury following endotoxin administration in rats. J Biomed Sci. 1999 Jan;6(1):28-35.