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1,3-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。
1,3-PBIT(dihydrobromide)图片
CAS NO:200716-66-1
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
potent inhibitor of iNOS
Cas No.200716-66-1
别名亚苯基-1,3-双(乙烷-2-异硫脲)二氢溴酸
化学名S,S'-1,3-phenylene-bis(1,2-ethanediyl)bis-isothiourea, dihydrobromide
Canonical SMILESN/C(SCCC1=CC(CCS/C(N)=N/[H])=CC=C1)=N/[H].Br.Br
分子式C12H18N4S2o 2HBr
分子量444.2
溶解度≤100mg/ml in Water
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

1,3-PBIT (dihydrobromide) is a potent and selective iNOS inhibitor with Ki value of 47 nM [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].

1,3-PBIT, also known as S,S’-(1,3-Phenylenebis(1,2-ethanediyl))bisisothiourea, is a potent and selective iNOS inhibitor. 1,3-PBIT inhibited purified human iNOS, eNOS and nNOS with Ki values of 47 nM, 9 μM and 0.25 μM, respectively. 1,3-PBIT exhibited 190-fold selective against iNOS versus eNOS. In DLD-1 cells, 1,3-PBIT inhibited human iNOS with IC50 value of 150 μM, presumably to poor membrane permeability [1].

In conscious male Sprague-Dawley rats, 1,3-PBIT (10mg/kg, ip; 1 h after endotoxin) inhibited endotoxin-induced decrease in MAP, renal CYP 4A1/A3 protein level and CYP 4A activity and increase in systemic and renal nitrite production [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].  Tunctan B, Yaghini FA, Estes A, et al. Inhibition by nitric oxide of cytochrome P450 4A activity contributes to endotoxin-induced hypotension in rats. Nitric Oxide. 2006 Feb;14(1):51-7.