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1400W 2HCl

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Chemical Structure| 214358-33-5 同义名 : 1400W (hydrochloride);N-(3-(Aminomethyl)benzyl)acetamidine;1400W Dihydrochloride
CAS号 : 214358-33-5
货号 : A269504
分子式 : C10H17Cl2N3
纯度 : 99%+
分子量 : 250.168
MDL号 : MFCD03428622
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(71.95 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(399.73 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • eNOS

    eNOS, Ki:50 μM

  • iNOS

    iNOS, Kd:<7 nM

  • nNOS

    nNOS, Ki:2 μM
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 Ks 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 Ki 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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.00mL

0.80mL

0.40mL

19.99mL

4.00mL

2.00mL

39.97mL

7.99mL

4.00mL
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.