MBP146-78
(Synonyms: 4-[2-(4-氟苯基)-5-(1-甲基-4-哌啶基)-1H-吡咯-3-基]吡啶) 目录号 : GC19240
MBP146-78 是一种有效的选择性 cGMP 依赖性蛋白激酶抑制剂。
Cas No.:188343-77-3
Sample solution is provided at 25 µL, 10mM.
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MBP146-78 is a potent and selective inhibitor of cGMP dependent protein kinases.
MBP146-78 displays a dose-dependent inhibition of T. gondii tachyzoites replicating inside HFFs, with an IC50 of 210 nM. The suppression of lytic parasite growth by MBP146-78 is reversible. Replacement of the medium with medium lacking MBP146-78, after treatment for up to 7 days at 2 uM, results in complete lysis of HFF cell monolayers. MBP146-78 is neither toxic nor inhibitory to proliferating or confluent monolayers of HFFs at concentrations of up to 10 uM[1].
In infected mice that are treated with MBP146-78 at 50 mg/kg twice daily, parasites are undetectable throughout the 10-day treatment period in each of the tissues examined. However, samples from brain, spleen, and lung taken from infected treated mice reveal the presence of parasites after cessation of administration of MBP146-78, indicating that a transient asymptomatic parasite recrudescence occurs in all survivors. The ability of mice to control Toxoplasma infection after MBP146-78 treatment has been terminated suggests that the mouse immune system plays a synergistic role with chemotherapy in controlling the infection[1].
References:
[1]. Nare B, et al. Evaluation of a cyclic GMP-dependent protein kinase inhibitor in treatment of murine toxoplasmosis: gamma interferon is required for efficacy. Antimicrob Agents Chemother. 2002 Feb;46(2):300-7.
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Cell experiment: |
To assess the toxicity of MBP146-78 to HFFs, cells are plated in 96-well plates at 1000/well and allowed to adhere overnight prior to addition of compound. Cultures are incubated for 5 days at 37°C in the presence of 5% CO2. Viability is assessed using the Cell-Titer 96 Aqueous One solution cell-proliferating assay[1]. |
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Animal experiment: |
Mice: MBP146-78 is dissolved in water. MBP146-78 is administered in 100 μL doses by intraperitoneal injections starting 24 h after parasite inoculation. Mice are monitored twice daily for clinical evidence of toxoplasmosis and mortality throughout the experimental period[1]. |
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References: [1]. Nare B, et al. Evaluation of a cyclic GMP-dependent protein kinase inhibitor in treatment of murine toxoplasmosis: gamma interferon is required for efficacy. Antimicrob Agents Chemother. 2002 Feb;46(2):300-7. |
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| Cas No. | 188343-77-3 | SDF | |
| 别名 | 4-[2-(4-氟苯基)-5-(1-甲基-4-哌啶基)-1H-吡咯-3-基]吡啶 | ||
| Canonical SMILES | CN1CCC(C2=CC(C3=CC=NC=C3)=C(C4=CC=C(F)C=C4)N2)CC1 | ||
| 分子式 | C21H22FN3 | 分子量 | 335.42 |
| 溶解度 | DMSO : 7.69 mg/mL (22.93 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 | 2.9813 mL | 14.9067 mL | 29.8134 mL |
| 5 mM | 0.5963 mL | 2.9813 mL | 5.9627 mL |
| 10 mM | 0.2981 mL | 1.4907 mL | 2.9813 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet