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S-ethyl N-[4-(trifluoromethyl)phenyl] Isothiourea(hydrochloride)
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。
S-ethyl N-[4-(trifluoromethyl)phenyl] Isothiourea(hydrochloride)图片
CAS NO:163490-78-6
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
100mg电议

产品介绍
selective, competitive inhibitor of nNOS
Cas No.163490-78-6
别名S-乙基-N-[4-(三氟甲基)苯基]异硫脲盐酸盐,EPIT
化学名ethyl[4-(trifluoromethyl)phenyl] carbamimidothioate, hydrochloride
Canonical SMILESCCS/C(N([H])C1=CC=C(C(F)(F)F)C=C1)=N\[H].Cl
分子式C10H11F3N2S o HCl
分子量284.7
溶解度≤34mg/ml in ethanol;34mg/ml in DMSO;34mg/ml in dimethyl formamide;50mg/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

S-ethyl N-[4-(trifluoromethyl)phenyl] Isothiourea (hydrochloride) is a selective and competitive nNOS inhibitor with Ki value of 0.32 μM for the purified human enzyme [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].

S-ethyl N-[4-(trifluoromethyl)phenyl] Isothiourea (hydrochloride) (EPIT) is a selective and competitive nNOS inhibitor. S-ethyl N-[4-(trifluoromethyl)phenyl] Isothiourea inhibited human nNOS, eNOS and iNOS with Ki values of 0.32 μM, 9.4 μM and 37 μM, respectively. EPIT exhibited 115-fold and 29-fold selectivity for nNOS compared to iNOS and eNOS, respectively [1].

In mice, EPIT administered intravenously at 25 mg/kg readily penetrated the blood-brain barrier, immediately reaching concentrations in the brain equal to the plasma concentration. In rat brain slices, EPIT failed to inhibit nNOS activity, possibly due to reduced intracellular uptake [1].

Reference:
[1].  Shearer BG, Lee S, Oplinger JA, et al. Substituted N-phenylisothioureas: potent inhibitors of human nitric oxide synthase with neuronal isoform selectivity. J Med Chem. 1997 Jun 6;40(12):1901-5.