Istradefylline-13C-d3
(Synonyms: KW-6002-13C,d3) 目录号 : GC47472
A neuropeptide with diverse biological activities
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Istradefylline-13C-d3 is intended for use as an internal standard for the quantification of istradefylline by GC- or LC-MS. Istradefylline is an adenosine receptor 2A (A2A) antagonist (Ki = 2.2 nM in a radioligand binding assay).1 In vivo, istradefylline inhibits catalepsy induced by haloperidol with an ED50 value of 0.23 mg/kg in rats. Oral administration of istradefylline alleviates postural defects in a dose-dependent manner without inducing dyskinesias or hyperactivity in an MPTP-induced marmoset model of Parkinson's disease.2 It also decreases bradykinesias induced by L-DOPA and improves attentional and working memory deficits in an MPTP-induced macaque model of Parkinson's disease.3 Formulations containing istradefylline are used to extend on-time in Parkinson's disease patients experiencing motor fluctuations.
1.Shimada, J., Nobuaki, K., Nonaka, H., et al.Adenosine A2A antagonists with potent anti-cataleptic activityBioorg. Med. Chem. Lett.7(18)2349-2352(1997) 2.Kanda, T., Jackson, M.J., Smith, L.A., et al.Adenosine A2A antagonist: A novel antiparkinsonian agent that does not provoke dyskinesia in parkinsonian monkeysAnn. Neurol.43(4)507-513(1998) 3.Ko, W.K.D., Camus, S.M., Li, Q., et al.An evaluation of istradefylline treatment on Parkinsonian motor and cognitive deficits in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated macaque modelsNeuropharmacology100(Pt. A)48-58(2016)
| Cas No. | N/A | SDF | |
| 别名 | KW-6002-13C,d3 | ||
| Canonical SMILES | CCN(C(N1CC)=O)C2=C(N([13C]([2H])([2H])[2H])C(/C=C/C3=CC=C(OC)C(OC)=C3)=N2)C1=O | ||
| 分子式 | C19[13C]H21D3N4O4 | 分子量 | 388.5 |
| 溶解度 | DMSO: soluble,Methanol: soluble | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.574 mL | 12.87 mL | 25.74 mL |
| 5 mM | 0.5148 mL | 2.574 mL | 5.148 mL |
| 10 mM | 0.2574 mL | 1.287 mL | 2.574 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。