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1400W二盐酸盐

1400W二盐酸盐用途

1400W dihydrochloride是高效,选择性的诱导型一氧化氮合成酶 (NO synthase) 抑制剂,Ki 值为7 nM。

1400W二盐酸盐名称

[ CAS 号 ]:
214358-33-5

[ 中文名 ]:
N-[3-(氨甲基)苄基]二盐酸乙脒

[ 英文名 ]:
1400W dihydrochloride

[英文别名 ]:

1400 W dihydrochloride
MFCD03428622
1400W dihydrochloride
1400W (Dihydrochloride)

1400W二盐酸盐生物活性

[ 描述 ]:

1400W dihydrochloride是高效,选择性的诱导型一氧化氮合成酶 (NO synthase) 抑制剂,Ki 值为7 nM。

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 一氧化氮合酶

研究领域 >> 心血管疾病

研究领域 >> 炎症/免疫

[ 靶点 ]

Ki: 7 nM (iNOS), 2 µM (nNOS), 50 µM (eNOS)[1]

[体外研究]

1400W是人诱导型一氧化氮合酶(iNOS)的缓慢,紧密结合抑制剂。 1400W的缓慢起效显示饱和动力学,最大速率常数为0.028s-1,结合常数为2.0μM。抑制依赖于辅因子NADPH。对于iNOS而言,1400W对eNOS的选择性至少为5000倍。相反,人神经元NOS和内皮NOS(eNOS)的抑制相对较弱,可快速逆转,并且与L-精氨酸竞争,Ki值分别为2μM和50μM[1]。 1400W处理抑制iNOS表达而不影响nNOS或eNOS。 1400W还可以减少NO,3-NT和MDA的产生,并防止大脑皮层神经细胞凋亡[2]。

[体内研究]

有效的1400W(ED50 = 0.3mg/kg)可减少由LPS诱导的iNOS引起的大鼠延迟性血管损伤,但与LPS同时给药时不会加剧急性血管渗漏[1]。 1400W的施用降低了所有实验组中的NOx水平。此外,脂质过氧化,凋亡细胞百分比和硝化蛋白表达在缺氧后期(48小时和5天)下降[3]。

[动物实验]

大鼠：通过测定[125I]人血清白蛋白从血浆到器官的渗漏，评估1400W对血浆渗漏的影响。将1400W（0.1-10mg / kg，皮下）溶解在等渗盐水中，并与内毒素同时施用或在LPS施用后3小时施用（大肠杆菌LPS，3mg / kg静脉内施用）。然后在输送1400W后1或5小时评估等离子体泄漏[1]。

[参考文献]

[1]. Garvey EP, 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 Feb 21;272(8):4959-63.

[2]. Shi Q, et al. 1400W ameliorates acute hypobaric hypoxia/reoxygenation-induced cognitive deficits by suppressing the induction of inducible nitric oxide synthase in rat cerebral cortex microglia. Behav Brain Res. 2017 Feb 15;319:188-199.

[3]. Rus A, et al. Inducible NOS inhibitor 1400W reduces hypoxia/re-oxygenation injury in rat lung. Redox Rep. 2010;15(4):169-78.

[相关活性小分子]

1400W二盐酸盐物理化学性质

[ 沸点 ]:
329ºC at 760 mmHg

[ 分子式 ]:
C₁₀H₁₇Cl₂N₃

[ 分子量 ]:
250.168

[ 闪点 ]:
152.7ºC

[ 精确质量 ]:
249.079956

[ PSA ]:
61.90000

[ LogP ]:
4.02700

[ 外观性状 ]:
粉末

[ 蒸汽压 ]:
0.000183mmHg at 25°C

[ 储存条件 ]:
-20℃

1400W二盐酸盐MSDS

详细MSDS(安全技术说明书)

1400W二盐酸盐安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

1400W二盐酸盐文献

NOS1-dependent negative feedback regulation of the epithelial sodium channel in the collecting duct.

Am. J. Physiol. Renal Physiol. 308(3) , F244-51, (2015)

With an increase in urine flow there is a significant increase in shear stress against the renal epithelium including the inner medullary collecting duct, resulting in an increase in nitric oxide (NO)...

Gardenamide A Protects RGC-5 Cells from H₂O₂-Induced Oxidative Stress Insults by Activating PI3K/Akt/eNOS Signaling Pathway.

Int. J. Mol. Sci. 16 , 22350-67, (2015)

Gardenamide A (GA) protects the rat retinal ganglion (RGC-5) cells against cell apoptosis induced by H₂O₂. The protective effect of GA was completely abrogated by the specific phosphoinositide 3-kinas...

Selective inhibition of inducible nitric oxide synthase inhibits tumor growth in vivo: studies with 1400W, a novel inhibitor.

Cancer Res. 57 , 3300, (1997)

We have investigated the effect of N-(3-(aminomethyl)benzyl)acetamidine (1400W), a novel and highly selective inhibitor for inducible NOS (iNOS), on in vivo growth of solid tumors expressing iNOS. For...

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