Proxyphylline
(Synonyms: 羟丙茶碱) 目录号 : GC10475
A methylxanthine derivative and an adenosine receptor antagonist
Cas No.:603-00-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ki: 82 nM for bovine brain A1 adenosine receptor
Proxyphylline is an A1 adenosine receptor antagonist.
The A1 adenosine receptor, the best characterized purinergic receptor family, can mediate responses via multiple pertussis toxin-sensitive GTP binding proteins to various different effectors.
In vitro: Previous study showed that proxyphylline could selectively antagonize A1 adenosine receptors versus A2 adenosine receptors (Ki = 850 μM for platelets) [1].
In vivo: In a previous study, rats that were allodynic following the vincristine injections were randomly allocated into four groups. Theoesberiven F (a combination of proxyphylline and Melilotus extract) was administered to rats. Results showed that the decreased paw withdrawal threshold induced by vincristine injection was increased by theoesberiven F treatment and the increased withdrawal frequency to cold stimuli was also reduced by theoesberiven F treatment [2].
Clinical trial: The proxyphylline PK was measured in healthy adults after intravenous, single oral and multiple oral doses to produce steady state. The mean peak time after oral administration was 29 min. The apparent volume of distribution was 0.611/kg. The ranges of biological half-life were 8.1-12.1 h and 8.3-12.6 h calculated from serum and urine data, respectively. In additioin, 24% of the dose was excreted in urine, which agreed with the relationship between the calculated total body clearance and the renal clearance of the drug [3].
References:
[1] U. Schwabe, D. Ukena and M. J. Lohse. Xanthine derivatives as antagonists at A1 and A2 adenosine receptors. Naunyn-Schmiedeberg's Arch.Pharmacol. 330,212-221 (1985).
[2] S. Bang, Y. S. Kim and S. R. Jeong. Anti-allodynic effect of theoesberiven F in a vincristine-induced neuropathy model. Exp. Ther. Med. 12(2), 799-803 (2016).
[3] Selvig K. Pharmacokinetics of proxyphylline in adults after intravenous and oral administration. Eur J Clin Pharmacol. 1981 Jan;19(2):149-55.
| Cas No. | 603-00-9 | SDF | |
| 别名 | 羟丙茶碱 | ||
| 化学名 | 3,7-dihydro-7-(2-hydroxypropyl)-1,3-dimethyl-1H-purine-2,6-dione | ||
| Canonical SMILES | CN(C(N1C)=O)C2=C(N(CC(O)C)C=N2)C1=O | ||
| 分子式 | C10H14N4O3 | 分子量 | 238.2 |
| 溶解度 | ≥ 10.1mg/mL 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 | 4.1982 mL | 20.9908 mL | 41.9815 mL |
| 5 mM | 0.8396 mL | 4.1982 mL | 8.3963 mL |
| 10 mM | 0.4198 mL | 2.0991 mL | 4.1982 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。