1400W dihydrochloride
(Synonyms: N-[3-(氨甲基)苄基]乙脒二盐酸盐) 目录号 : GC13563
A potent, selective iNOS inhibitor
Cas No.:214358-33-5
Sample solution is provided at 25 µL, 10mM.
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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.
| Kinase experiment [1]: | |
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Kinase assays |
The oxidation of L-[14C]arginine was monitored by the conversion of L-[14C]arginine to L-[14C]citrulline. The enzyme was assayed at 37°C in 20 mM Hepes, pH 7.4, with 2.5 mM dithiothreitol, 125 μM NADPH, 10 μM tetrahydrobiopterin, 10 μM FAD, and 0.5-20 μM L-[14C]arginine (10,000 cpm). When eNOS or nNOS were assayed, calmodulin (10 μg/ml) and CaCl2 (2.5 mM) were included. When time courses were measured, bovine serum albumin (1 mg/ml) was included. |
| Animal experiment [1]: | |
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Animal models |
Rat model of endotoxin-induced microvascular injury |
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Dosage form |
0.1-10 mg/kg, subcutaneous |
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Application |
1400W was a potent inhibitor against iNOS in a rat model of endotoxin-induced vascular injury. When administered 3 h after endotoxin, 1400W completely suppressed leakage into the ileum. 1400W has an effect of endotoxin -induced vascular injury in the ileum. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. | |
| Cas No. | 214358-33-5 | SDF | |
| 别名 | N-[3-(氨甲基)苄基]乙脒二盐酸盐 | ||
| 化学名 | (E)-N'-(3-(aminomethyl)benzyl)acetimidamide dihydrochloride | ||
| Canonical SMILES | NCC1=CC(C/N=C(C)/N)=CC=C1.Cl.Cl | ||
| 分子式 | C10H15N3.2HCl | 分子量 | 250.17 |
| 溶解度 | ≥ 25mg/mL in DMSO | 储存条件 | Desiccate at RT |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.9973 mL | 19.9864 mL | 39.9728 mL |
| 5 mM | 0.7995 mL | 3.9973 mL | 7.9946 mL |
| 10 mM | 0.3997 mL | 1.9986 mL | 3.9973 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet