S-ethyl N-[4-(trifluoromethyl)phenyl] Isothiourea(hydrochloride)

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CAS NO:

163490-78-6

包装与价格：

包装	价格(元)
10mg	询价
25mg	询价
100mg	询价

化学性质

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	284.7
Cas No.	163490-78-6
Formula	C₁₀H₁₁F₃N₂S·HCl
Synonyms	EPIT
Solubility	≤34mg/ml in ethanol;34mg/ml in DMSO;34mg/ml in dimethyl formamide;50mg/ml in H2O
Chemical Name	ethyl[4-(trifluoromethyl)phenyl] carbamimidothioate, hydrochloride
Canonical SMILES	CCS/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.