1. Anti-infection
  2. Parasite
  3. MBP146-78

MBP146-78 

Cat. No.: HY-101525 Purity: 99.19%
Handling Instructions

MBP146-78 is a potent and selective inhibitor of cGMP dependent protein kinases.

For research use only. We do not sell to patients.

MBP146-78 Chemical Structure

MBP146-78 Chemical Structure

CAS No. : 188343-77-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 97 In-stock
Estimated Time of Arrival: December 31
1 mg USD 84 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
25 mg USD 396 In-stock
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

MBP146-78 is a potent and selective inhibitor of cGMP dependent protein kinases.

In Vitro

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 μM, 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 μM[1].

In Vivo

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].

Molecular Weight

335.42

Formula

C₂₁H₂₂FN₃

CAS No.

188343-77-3

SMILES

CN1CCC(C2=CC(C3=CC=NC=C3)=C(C4=CC=C(F)C=C4)N2)CC1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 7.69 mg/mL (22.93 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.77 mg/mL (2.30 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.77 mg/mL (2.30 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.77 mg/mL (2.30 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Product Name:
MBP146-78
Cat. No.:
HY-101525
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