1400W dihydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
1400W dihydrochloride是一种强效的和选择性的诱导型一氧化氮合酶抑制剂,Kd值为7 nM [1].
诱导型一氧化氮合酶(iNOS)是一种催化产生一氧化氮(NO)的酶并参与免疫应答.iNOS产生NO作为一种免疫防御机制.
1400W dihydrochloride是一种非常缓慢可逆的和选择性的iNOS抑制剂[1].1400W抑制iNOS,Kd值为7 nM,并迅速可逆地抑制人类神经NOS(nNOS)和内皮NOS(eNOS),Ki值分别为2和50 μM.L-精氨酸是一种竞争性的1400W抑制剂,Ks值为3.0 μM[1].
在内毒素诱导血管损伤的大鼠模型中,1400W对iNOS表现出比eNOS强50倍的选择性[1].在局灶脑缺血大鼠中,1400W (20 mg/kg)抑制神经功能障碍和体重减轻,并显著减少缺血性病变体积达31%.另外,1400W减少梗死中iNOS活性达36%[2].在EMT6小鼠乳腺癌中,1400W (10 或12 mg/kg/h)显著降低肿瘤重量并抑制iNOS活性[3].
参考文献:
[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, Bhme GA, Lerouet D, et al. Selective inhibition of inducible nitric oxide synthase prevents ischaemic brain injury. Br J Pharmacol, 1999, 127(2): 546-552.
Storage | Desiccate at RT |
M.Wt | 250.17 |
Cas No. | 214358-33-5 |
Formula | C10H15N3·2HCl |
Solubility | ≥25 mg/mL in DMSO; insoluble in EtOH; ≥23.2 mg/mL in H2O |
Chemical Name | (E)-N'-(3-(aminomethyl)benzyl)acetimidamide dihydrochloride |
SDF | Download SDF |
Canonical SMILES | NCC1=CC(C/N=C(C)/N)=CC=C1.Cl.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。 |
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. |
质量控制和MSDS
- 批次: