MBP146-78 |
| Catalog No.GC19240 |
MBP146-78은 cGMP 의존성 단백질 키나제의 강력하고 선택적인 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Canonical SMILES | CN1CCC(C2=CC(C3=CC=NC=C3)=C(C4=CC=C(F)C=C4)N2)CC1 | ||
| Formula | C21H22FN3 | M.Wt | 335.42 |
| Solubility | DMSO : 7.69 mg/mL (22.93 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)
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