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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)
10mg电议
25mg电议
100mg电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt284.7
Cas No.163490-78-6
FormulaC10H11F3N2S·HCl
SynonymsEPIT
Solubility≤34mg/ml in ethanol;34mg/ml in DMSO;34mg/ml in dimethyl formamide;50mg/ml in H2O
Chemical Nameethyl[4-(trifluoromethyl)phenyl] carbamimidothioate, hydrochloride
Canonical SMILESCCS/C(N([H])C1=CC=C(C(F)(F)F)C=C1)=N\[H].Cl
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

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.