|N-(3-(氨甲基)苄基)乙脒二盐酸盐|CsnPharm

CAS No.: 214358-33-5

1400W 2HCl Catalog No. CSN16858

Synonyms: N-(3-(Aminomethyl)benzyl)acetamidine;1400W (hydrochloride);1400W HCl

1400W 2HCl is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase (iNOS).

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技术信息

生物活性

描述Nitric oxide synthase (NOS) catalyzes the formation of nitric oxide and L-citrulline from L-arginine. 1400W 2HCl is a slow, tight binding, selective inhibitor of human inducible nitric-oxide synthase (iNOS). The apparent binding constant of 1400W 2HCl was 2.3 μM at an L-arginine concentration of 0.5 μM. The substrate L-arginine blocked the binding of 1400W 2HCl to iNOS with a K_s value of 3.0 μM. 1400W 2HCl is also a reversible and relatively inefficient inhibitor of human endothelial NOS (eNOS) and neuronal NOS (nNOS). Inhibition of eNOS and nNOS by 1400W 2HCl was competitive with L-arginine with K_i values of 50 μM and 2.0 μM, respectively. Moreover, 1400W 2HCl showed potent inhibitory activity in rat aortic rings with an EC₅₀ value of 0.8 μM^[3]. In RAW264.7 cells treated with LPS/IFNγ for 16h, the increased p53 and GAPDH acetylation was blocked by 1400W 2HCl at the concentration of 100 μM. The augmented p300 acetylation, GAPDH–p300 binding and GAPDH-p53 binding in RAW264.7 cells were also abolished by 100 μM 1400W 2HCl^[4]. In a rat model of endotoxin-induced microvascular injury, subcutaneous administration of 1400W 2HCl 3h after endotoxin completely suppressed the leakage into ileum with an ED₅₀ value of 0.16 mg/kg^[3].
作用机制1400W 2HCl is a tight binding, selective inhibitor of NOS. It is competitive with the substrate L-arginine.
参考文献

[1] Ersoz N, Guven A, et al. Comparison of the efficacy of melatonin and 1400W on renal ischemia/reperfusion injury: a role for inhibiting iNOS. Ren Fail. 2009;31(8):704-10.
[2] Garvey EP, Oplinger JA, 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.
[3] Garvey EP, Oplinger JA, Furfine ES, Kiff RJ, Laszlo F, Whittle BJ, Knowles RG. 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. doi: 10.1074/jbc.272.8.4959. PMID: 9030556.
[4] Sen N, Hara MR, Kornberg MD, Cascio MB, Bae BI, Shahani N, Thomas B, Dawson TM, Dawson VL, Snyder SH, Sawa A. Nitric oxide-induced nuclear GAPDH activates p300/CBP and mediates apoptosis. Nat Cell Biol. 2008 Jul;10(7):866-73. doi: 10.1038/ncb1747. Epub 2008 Jun 15. PMID: 18552833; PMCID: PMC2689382.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.9973 mL
- 19.9866 mL
- 39.9731 mL
- 5 mM
- 0.7995 mL
- 3.9973 mL
- 7.9946 mL
- 10 mM
- 0.3997 mL
- 1.9987 mL
- 3.9973 mL

技术信息

CAS号

214358-33-5

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C10H17Cl2N3

运输

蓝冰

分子量

250.17

别名

N-(3-(Aminomethyl)benzyl)acetamidine;1400W (hydrochloride);1400W HCl;1400W hydrochloride

溶解度

DMSO	115.0 mg/mL (459.7 mM)
Water	90.0 mg/mL (359.8 mM)

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1400W 2HCl Catalog No. CSN16858

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