ARL 17477 dihydrochloride
目录号 : GC14802
Selective nNOS inhibitor
Cas No.:866914-87-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
ARL 17477 dihydrochloride is a selective and potent neuronal nitrogen oxide synthase (nNOS) inhibitor with IC50 values of 1 and 17μM for nNOS and endothelial NOS, respectively [1].
Neuronal NOS (nNOS) plays an important role in the development of ischaemic brain necrosis while endothelial NOS (eNOS) protects brain tissue through increasing ischaemic regional cerebral blood flow [1].
In rats after transient MCA occlusion, ARL 17477 (1mg/kg, 3mg/kg and 10mg/kg) reduced ischemic infarct volume by 53%, 23% and 6.5% respectively in a dose-dependent way. ARL 17477 (10 mg/kg) significantly reduced regional cerebral blood flow (rCBF) by 27±5.3% and 24±14.08%. Also, it reduced cortical NOS activity by 86±14.9% and 91±8.9% at 10 min or 3 h, respectively [2]. In the global cerebral ischaemia gerbil model, the combination of MK-801 with ARL 17477 provided 44% greater protection than the total protection or either alone. Likewise, the combination of LY293558 with ARL 17477 provided 35% greater protection than total protection of either compound alone [3].
References:
[1]. O'Neill MJ, Murray TK, McCarty DR, et al. ARL 17477, a selective nitric oxide synthase inhibitor, with neuroprotective effects in animal models of global and focal cerebral ischaemia. Brain Res, 2000, 871(2): 234-244.
[2]. Zhang ZG, Reif D, Macdonald J, et al. ARL 17477, a potent and selective neuronal NOS inhibitor decreases infarct volume after transient middle cerebral artery occlusion in rats. J Cereb Blood Flow Metab, 1996, 16(4): 599-604.
[3]. Hicks CA, Ward MA, Swettenham JB, et al. Synergistic neuroprotective effects by combining an NMDA or AMPA receptor antagonist with nitric oxide synthase inhibitors in global cerebral ischaemia. Eur J Pharmacol, 1999, 381(2-3): 113-119.
| Cas No. | 866914-87-6 | SDF | |
| 化学名 | (Z)-N'-(4-(2-((3-chlorobenzyl)amino)ethyl)phenyl)thiophene-2-carboximidamide dihydrochloride | ||
| Canonical SMILES | ClC1=CC=CC(CNCCC2=CC=C(/N=C(N)/C3=CC=CS3)C=C2)=C1.Cl.Cl | ||
| 分子式 | C20H20ClN3S.2HCl | 分子量 | 442.83 |
| 溶解度 | <22.14mg/ml in Water; <44.28mg/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 | 2.2582 mL | 11.291 mL | 22.582 mL |
| 5 mM | 0.4516 mL | 2.2582 mL | 4.5164 mL |
| 10 mM | 0.2258 mL | 1.1291 mL | 2.2582 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。