BW-A 78U
目录号 : GC31915
BW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity.
Cas No.:101155-02-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | Mononuclear cells are incubated for 30 min with BW-A 78U at the concentration of 10 nM to 10 μM. The cells are then stimulated with lipopolysaccharide (10 μg/mL) overnight at 37°C in an atmosphere of 5% CO2 at 100% humidity. Cell-free supernatants are collected, centrifuged (2000 g), and stored frozen at -20°C before TNF-α determination. TNF-α concentrations in cell culture supernatants are determined by specific ELISA using a commercial kit. Sensitivity of the assay is 1 pg/mL. The absorbance at 450 nm is assessed with an ELISA reader[1]. |
References: [1]. Boichot E, et al. Anti-inflammatory activities of a new series of selective phosphodiesterase 4 inhibitors derivedfrom 9-benzyladenine. J Pharmacol Exp Ther. 2000 Feb;292(2):647-53. | |
BW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity.
| Cas No. | 101155-02-6 | SDF | |
| Canonical SMILES | CNC1=C2N=CN(CC3=CC=CC=C3F)C2=NC=N1 | ||
| 分子式 | C13H12FN5 | 分子量 | 257.27 |
| 溶解度 | DMSO : 150 mg/mL (583.05 mM) | 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 | 3.887 mL | 19.4348 mL | 38.8697 mL |
| 5 mM | 0.7774 mL | 3.887 mL | 7.7739 mL |
| 10 mM | 0.3887 mL | 1.9435 mL | 3.887 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。
Anxiolytic and sedative properties of BW A78U, a novel anticonvulsant adenine derivative
The anticonvulsant BW A78U, tested in a free mouse exploratory situation, reduced in a dose-dependent fashion the locomotion and the number of rearings, this sedative effect being significant up to a dose of 15 mg/kg (IP, 20 min before testing). In an unconditioned conflict test, the light/dark box choice situation, specific for anxiolytics, low doses of BW A78U increased the time spent by mice in the lit box as well as the number of transitions between the two boxes. Finally, we demonstrated that this drug was able to protect mice against pentylenetetrazole-induced convulsions. Our data show that BW A78U possesses some of the characteristic properties of the minor tranquilizers. However, since this compound binds to the benzodiazepine receptor with a very low affinity (IC50 = 13.6 microM), it can be assumed that this drug does not exert its behavioral effects through these receptors. It may interfere with other targets involving adenosine, another potent physiological regulator of neuronal excitability.
9-Benzyladenines: potent and selective cAMP phosphodiesterase inhibitors
Behavioral effects of rolipram and structurally related compounds in mice: behavioral sedation of cAMP phosphodiesterase inhibitors
The behavioral effects of specific cAMP phosphodiesterase inhibitors (PDE-I) such as rolipram and structurally related compounds were investigated in mice. Selected PDE-I induced a potent dose-dependent decrease in locomotion and in rearing of mice confronted with a free exploratory procedure, these effects being considered as a behavioral sedation. However, in the light/dark choice test especially conceived to reveal disinhibitory and/or anxiolytic action, they did not show obvious effects. These results suggest that the increase of cAMP probably does not account for our previously observed anxiolytic properties of BW A78U, an adenine derivative PDE-I (20).
Synthesis and anticonvulsant activity of N-benzylpyrrolo[2,3-d]-, -pyrazolo[3,4-d]-, and -triazolo[4,5-d]pyrimidines: imidazole ring-modified analogues of 9-(2-fluorobenzyl)-6-(methylamino)-9H-purine
Analogues of 9-(2-fluorobenzyl)-6-(methylamino)-9H-purine (1) containing isosteric replacements of the imidazole ring atoms were synthesized and tested for anticonvulsant activity. The pyrrolo[2,3-d]-, pyrazolo[3,4-d]-, and triazolo[4,5-d]pyrimidines were less active than 1 against maximal electroshock-induced seizures (MES) in rats when given po. The differences in anti-MES activity for these analogues was not explained by differences in pKa or lipophilicity. However, the four classes of heterocycles have distinctly different calculated electrostatic isopotential maps, which may be related to optimum anticonvulsant activity.