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| 25mg |
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MBP146-78 (MBP-146-78) is a potent and selective inhibitor of cGMP dependent protein kinases with the potential for the treatment of murine toxoplasmosis.
| Targets |
Toxoplasma
|
|---|---|
| ln Vitro |
MBP146-78 exhibits a dose-dependent inhibition of T. gondii tachyzoites replicating within HFF, with an IC50 of 210 nM. MBP146-78 has the ability to reverse the inhibition of lytic parasite growth. HFF cell monolayers are completely lysed when the medium containing MBP146-78 is substituted after up to seven days of treatment at a concentration of 2 μM. At concentrations of up to 10 μM, MBP146-78 neither inhibits nor is toxic to proliferating or confluent monolayers of HFFs[1].
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| ln Vivo |
Parasites are not visible in any of the tissues examined during the 10-day treatment period in mice that are infected and given MBP146-78 at a dose of 50 mg/kg twice daily. All survivors experience a brief period of asymptomatic parasite recrudescence, as evidenced by the presence of parasites in samples from the brain, spleen, and lung of infected treated mice, even after MBP146-78 administration has stopped. Following the cessation of MBP146-78 treatment, mice's ability to control Toxoplasma infection implies that chemotherapy and the mouse immune system work in concert to control the infection[1].
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| Cell Assay |
In order to evaluate the toxicity of MBP146-78 to HFFs, 1000 cells are plated in each well of 96-well plates, and the cells are left to adhere for the entire night before the compound is added. The cultures are kept in an incubator with 5% CO2 at 37°C for five days. The cell-proliferating assay in the Cell-Titer 96 Aqueous One solution is used to determine viability[1].
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| Animal Protocol |
Mice: In water, MBP146-78 dissolves. Intraperitoneal injections of 100 μL doses of MBP146-78 are given beginning 24 hours after parasite inoculation. Throughout the trial, mice are checked twice a day for signs of toxoplasmosis and mortality[1].
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| References | |
| Additional Infomation |
Pyridine, 4-[2-(4-fluorophenyl)-5-(1-methyl-4-piperidinyl)-1H-pyrrol-3-yl]- has been reported in Diaporthe with data available.
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| Molecular Formula |
C21H22FN3
|
|---|---|
| Molecular Weight |
335.4179
|
| Exact Mass |
335.18
|
| CAS # |
188343-77-3
|
| PubChem CID |
500899
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.629
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
25
|
| Complexity |
409
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
FC1C([H])=C([H])C(=C([H])C=1[H])C1=C(C2C([H])=C([H])N=C([H])C=2[H])C([H])=C(C2([H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C2([H])[H])N1[H]
|
| InChi Key |
RBWNFHXBUDPAIO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H22FN3/c1-25-12-8-16(9-13-25)20-14-19(15-6-10-23-11-7-15)21(24-20)17-2-4-18(22)5-3-17/h2-7,10-11,14,16,24H,8-9,12-13H2,1H3
|
| Chemical Name |
4-[2-(4-fluorophenyl)-5-(1-methylpiperidin-4-yl)-1H-pyrrol-3-yl]pyridine
|
| Synonyms |
MBP146-78
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~7.7~12 mg/mL (~22.9~35.8 mM)
Ethanol: ~12 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.77 mg/mL (2.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.77 mg/mL (2.30 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.77 mg/mL (2.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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