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1400W dihydrochloride

现货
Catalog No.
B6730
INOS抑制剂
组合的产品项目
规格价格库存 数量
10mg
¥ 750.00
现货
50mg
¥ 3,000.00
现货
100mg
¥ 4,800.00
现货

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Background

1400W dihydrochloride is a potent and selective inhibitor of inducible nitric oxide synthase with Kd value of 7 nM [1].

Inducible nitric oxide synthase (iNOS) is an enzyme catalyzing the production of nitric oxide (NO) and is involved in immune response. iNOS produces NO as an immune defense mechanism.

1400W dihydrochloride is an extremely slowly reversible and selective iNOS inhibitor [1]. 1400W inhibited iNOS with Kd value of 7 nM and rapidly reversibly inhibited human neuronal NOS (nNOS) and endothelial NOS (eNOS) with Ki values of 2 and 50 μM, respectively. L-arginine was a competitive inhibitor of 1400W with Ks value of 3.0 μM [1].

In an endotoxin-induced vascular injury rat model, 1400W exhibited 50-fold more potent selectivity against iNOS than eNOS [1]. In focal cerebral ischaemia rats, 1400W (20 mg/kg) inhibited neurological dysfunction and weight loss and significantly decreased ischaemic lesion volume by 31%. Also, 1400W reduced iNOS activity by 36% in the infarct [2]. In the EMT6 murine mammary adenocarcinoma, 1400W (10 or 12 mg/kg/h) significantly reduced tumor weight and inhibited iNOS activity [3].

References:
[1].  Garvey EP, Oplinger JA, Furfine ES, et al. 1400W is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase in vitro and in vivo. J Biol Chem, 1997, 272(8): 4959-4963.
[2].  Thomsen LL, Scott JM, Topley P, et al. Selective inhibition of inducible nitric oxide synthase inhibits tumor growth in vivo: studies with 1400W, a novel inhibitor. Cancer Res, 1997, 57(15): 3300-3304.
[3].  Parmentier S, Böhme GA, Lerouet D, et al. Selective inhibition of inducible nitric oxide synthase prevents ischaemic brain injury. Br J Pharmacol, 1999, 127(2): 546-552.

Chemical Properties

StorageDesiccate at RT
M.Wt250.17
Cas No.214358-33-5
FormulaC10H15N3.2HCl
Solubility≥25mg/mL in DMSO
Chemical Name(E)-N'-(3-(aminomethyl)benzyl)acetimidamide dihydrochloride
SDFDownload SDF
Canonical SMILESNCC1=CC(C/N=C(C)/N)=CC=C1.Cl.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
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。

试验操作

酶学实验[1]:

激酶检测

通过L-[14C]精氨酸转化为L-[14C]瓜氨酸来监测L-[14C]精氨酸的氧化。在37℃下,用2.5mM二硫苏糖醇,125μM NADPH,10μM四氢生物蝶呤,10μM FAD和0.5-20μM L-[14C]精氨酸(10,000cpm)在20mM Hepes,pH 7.4中测定酶活。当测定eNOS或nNOS时,添加钙调蛋白(10μg/ml)和CaCl2(2.5mM)。测量时,添加牛血清白蛋白(1mg/mL)。

动物实验[1]:

动物模型

内毒素诱导的微血管损伤大鼠模型

剂量

0.1-10 mg/kg,皮下注射

应用

在内毒素诱导的微血管损伤大鼠模型中,1400W是iNOS的有效抑制剂,在施加内毒素3小时后,1400W可完全抑制回肠漏液。1400W在大鼠回肠中具有抗内毒素诱导的血管损伤的作用。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Garvey EP, Oplinger JA, Furfine ES, et al. 1400W is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase in vitro and in vivo. J Biol Chem, 1997, 272(8): 4959-4963.

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