L-NIL hydrochloride
目录号 : GC15807
L-NIL hydrochloride 是一种诱导型 NO 合酶抑制剂，对 miNOS 的 IC50 为 3.3 μM。
Cas No.:159190-45-1;150403-89-7
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
L-NIL is a potent and selective inhibitor of inducible NO synthase with IC50s of 3.3 and 92 μM for mouse inducible NO synthase and rat brain constitutive NO synthase, respectively.
L-NIL produces a concentration-dependent inhibition of both the mouse inducible NOS (miNOS) and the rat brain constitutive NOS (rcNOS) and is considerably more potent for miNOS. The IC50 values for L-NIL with miNOS and rcNOS are 3.3 and 92 pM, respectively, indicating that L-NIL is 28-fold more selective for miNOS. In addition, L-NIL has approximately 6-fold greater potency for miNOS than either L-NMA or L-NNA[1].
L-NIL may prove particularly useful in determining the role of nitric oxide production by inducible NOS in models of chronic inflammation (e.g., adjuvant arthritis)[1]. L-NIL suppresses the increase in plasma nitrite levels and joint inflammation associated with adjuvant-induced arthritis in a dose-dependent manner. L-NIL attenuates the inducible nitric oxide synthase immunoreactivity in adjuvant-treated rats. L-NIL protects the integrity of the tarsal, talus and calcaneus bones as well as the soft tissue surrounding the joint, while adjuvant controls exhibit severe deterioration of these bones and dramatic soft tissue swelling[2]. L-NIL limits progression of preexisting atherosclerosis in hypercholesterolemic rabbits. Increased intimal collagen accumulation may participate in iNOS-induced atherosclerosis progression[3].
References:
[1]. Moore WM, et al. L-N6-(1-iminoethyl)lysine: a selective inhibitor of inducible nitric oxide synthase. J Med Chem. 1994 Nov 11;37(23):3886-8.
[2]. Connor JR, et al. Suppression of adjuvant-induced arthritis by selective inhibition of inducible nitric oxide synthase. Eur J Pharmacol. 1995 Jan 24;273(1-2):15-24.
[3]. Behr-Roussel D, et al. Effect of chronic treatment with the inducible nitric oxide synthase inhibitor N-iminoethyl-L-lysine or with L-arginine on progression of coronary and aortic atherosclerosis in hypercholesterolemic rabbits. Circulation. 2000 Aug 29;102(9):1033-8.
|
Animal experiment: |
Rats: Nitric oxide synthase inhibitors are administered either by i.v. infusion or in the drinking water. For i.v. infusion of the inhibitors, aminoguanidine (3 M in buffered saline) or L-NIL (1 M in buffered saline) is administered using an osmotic minipump cannulated to the jugular vein beginning the same day as adjuvant administration. When added to the drinking water, aminoguandine is given at a dose of I mg/mL and L-NIL is given at a dose range of 1-100 μg /mL beginning 3 days prior to adjuvant administration. At the end of the experiment, the left femoral artery is cannulated and systemic blood pressure is measured in conscious, restrained animals[2]. |
|
References: [1]. Moore WM, et al. L-N6-(1-iminoethyl)lysine: a selective inhibitor of inducible nitric oxide synthase. J Med Chem. 1994 Nov 11;37(23):3886-8. |
|
| Cas No. | 159190-45-1;150403-89-7 | SDF | |
| 化学名 | (S,E)-2-amino-6-((1-aminoethylidene)amino)hexanoic acid hydrochloride | ||
| Canonical SMILES | OC([C@H](CCCC/N=C(C)/N)N)=O.Cl | ||
| 分子式 | C8H17N3O2.HCl | 分子量 | 223.7 |
| 溶解度 | <22.37mg/ml in Water | 储存条件 | Desiccate at -20°C |
| 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 4.4703 mL | 22.3514 mL | 44.7027 mL |
| 5 mM | 0.8941 mL | 4.4703 mL | 8.9405 mL |
| 10 mM | 0.447 mL | 2.2351 mL | 4.4703 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet