TS-011
(Synonyms: N-(3-氯-4-吗啉代苯基)-N'-羟基甲脒) 目录号 : GC32657
An inhibitor of 20-HETE synthesis
Cas No.:339071-18-0
Sample solution is provided at 25 µL, 10mM.
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TS-011 is an inhibitor of 20-hydroxyeicosatetraenoic acid (20-HETE) synthesis.1 It inhibits 20-HETE synthesis in human and rat renal microsomes (IC50s = 8.42 and 9.19 nM, respectively), as well as by the cytochrome P450 (CYP) isoforms CYP4F2, CYP4F3A, CYP4F3B, and CYP4A11 in cell-free assays (IC50s = 30.4, 42.6, 43.0, and 188 nM, respectively). It is selective for these CYPs over CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 (IC50s = >60 ?M for all), as well as a panel of receptors and other enzymes at 1 ?M. TS-011 (0.01-1 mg/kg, i.v.) reverses decreases in cerebral blood flow and increases in cerebrospinal fluid 20-HETE levels in a rat model of subarachnoid hemorrhage. It also reduces infarct volume and prevents neurological deficits in a rat model of stroke induced by middle cerebral artery occlusion (MCAO).2
1.Miyata, N., Seki, T., Tanaka, Y., et al.Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic strokeJ. Pharmacol. Exp. Ther.314(1)77-85(2005) 2.Omura, T., Tanaka, Y., Miyata, N., et al.Effect of a new inhibitor of the synthesis of 20-HETE on cerebral ischemia reperfusion injuryStroke37(5)1307-1313(2006)
Animal experiment: | The studies are performed using 58 male C57BL/6J mice (8 weeks old) weighing 20 to 26 g. TS-011 (0.3 mg/kg) or a vehicle is infused intravenously for 1 h every 6 h in a mouse model of stroke, induced by transient occlusion of the middle cerebral artery occlusion following photothrombosis. The cerebral blood flow velocity and the vascular perfusion area of the peri-infarct microvessels are measured using in vivo two-photon imaging[1]. |
References: [1]. Marumo T, et al. The inhibitor of 20-HETE synthesis, TS-011, improves cerebral microcirculatory autoregulation impaired by middle cerebral artery occlusion in mice. Br J Pharmacol. 2010 Nov;161(6):1391-402. | |
| Cas No. | 339071-18-0 | SDF | |
| 别名 | N-(3-氯-4-吗啉代苯基)-N'-羟基甲脒 | ||
| Canonical SMILES | ClC(C=C(/N=C/NO)C=C1)=C1N2CCOCC2 | ||
| 分子式 | C11H14ClN3O2 | 分子量 | 255.7 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store 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。 |
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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 | 3.9108 mL | 19.5542 mL | 39.1083 mL |
| 5 mM | 0.7822 mL | 3.9108 mL | 7.8217 mL |
| 10 mM | 0.3911 mL | 1.9554 mL | 3.9108 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet