UK-240455
目录号 : GC31153
UK-240455是一个有效且有选择性的N-甲基D-天冬氨酸(NMDA)甘氨酸位点上的拮抗剂。
Cas No.:178908-09-3
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
Animal experiment: | UK-240455 is administered both i.v. and orally at a dose of 2 mg/kg to male rats. Before and during the i.v. and oral studies, animals have free access to food and water. For i.v. studies, UK-240455 is administered to rats (250 to 300 g) via the tail vein. At the following time points (n=3/time point) blood samples are taken under terminal anaesthesia: predose, 0.1, 0.25, 0.5, 1.0, 1.5, 2.0, 4.0 and 7.0 h postdose. Blood samples are collected into heparinized tubes and centrifuged to separate plasma. The plasma is removed and stored frozen. Three further rats are dosed with UK-240455 as above and placed in metabolism cages to collect urine. After 24 h, these animals are killed and the urine collected and stored frozen[1]. |
References: [1]. Webster R, et al. Pharmacokinetics and disposition of a novel NMDA glycine site antagonist (UK-240,455) in rats, dogs and man. Xenobiotica. 2003 May;33(5):541-60. | |
UK-240455 is a potent and selective N-methyl D-aspartate (NMDA) glycine site antagonist.
UK-240455 is a potent and selective N-methyl D-aspartate (NMDA) glycine site antagonist. Following i.v. administration of UK-240455 to male rats, UK-240455 has a clearance of 12 mL/min/kg and a volume of distribution of 0.4 L/kg. The plasma concentration of UK-240455 decreases with an apparent half-life of 0.4 h. Analysis of urine (0 to 24 h) for unchanged UK-240455 indicates that 57% of the dose administered is excreted unchanged in the urine. The urinary clearance of UK-240455 in the rat is therefore 7 mL/min/kg. Following oral administration of UK-240455 to male rats, the apparent elimination half-life of UK-240455 from plasma following oral administration is 1.6 h[1].
[1]. Webster R, et al. Pharmacokinetics and disposition of a novel NMDA glycine site antagonist (UK-240,455) in rats, dogs and man. Xenobiotica. 2003 May;33(5):541-60.
| Cas No. | 178908-09-3 | SDF | |
| Canonical SMILES | CS(=O)(N(C1=C(Cl)C(Cl)=CC(NC2=O)=C1NC2=O)CCO)=O | ||
| 分子式 | C11H11Cl2N3O5S | 分子量 | 368.19 |
| 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 | 2.716 mL | 13.5799 mL | 27.1599 mL |
| 5 mM | 0.5432 mL | 2.716 mL | 5.432 mL |
| 10 mM | 0.2716 mL | 1.358 mL | 2.716 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。