TgCDPK1-IN-1
TgCDPK1-IN-1 is an orally active, blood-brain barrier-permeable TgCDPK1 inhibitor (IC50 = 15.7 nM) with antiparasitic activity against Toxoplasma gondii. TgCDPK1-IN-1 inhibits Src and TgCDPKG128M. TgCDPK1-IN-1 cures acute toxoplasmosis in immunocompetent mice and prolongs the survival of immunocompromised mice. TgCDPK1-IN-1 is applicable for research related to toxoplasmosis.
For research use only. We do not sell to patients.
- Formula: C18H13F3N8O
- Molecular Weight:414.34
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Biological Activity
Description
In Vitro
TgCDPK1-IN-1 (Compound 16c) inhibits the proliferation of Toxoplasma gondii tachyzoites in human foreskin fibroblasts (HFF cells), with an EC50 value of 270 nM[1].
TgCDPK1-IN-1 (10 μM) inhibits the activity of Src kinase by 18.2%[1].
TgCDPK1-IN-1 (20 μM) inhibits the kinase activity of the TgCDPK1G128M mutant by 13.6%[1].
TgCDPK1-IN-1 (20 μM) induces 8.6% cytotoxicity in HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
In Vivo
TgCDPK1-IN-1 (16c) (30-100 mg/kg; p.o.; 1-2 times daily; for 14 consecutive days) significantly prolongs the survival time of immunodeficient Ifngr1−/− mice infected with toxoplasmosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (immunocompetent; infected via i.p. injection with ME49-FLUC Toxoplasma gondii)[1]
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Dosage:30 mg/kg; 100 mg/kg
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Administration:p.o.; twice daily; p.o.; once daily
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Result:Achieved 100% survival but persistent chronic infection in all 5 treated mice at 30 mg/kg twice daily.
Achieved 100% survival and no evidence of chronic infection (cure) in all 5 treated mice at 100 mg/kg once daily.
Showed better control of infection (lower bioluminescence signals, more rapid weight recovery) in mice treated with 100 mg/kg once daily compared to those treated with 30 mg/kg twice daily.
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Animal Model:Ifngr1−/− mice (immunocompromised; infected via oral gavage with 5 tissue cysts of ME49-FLUC Toxoplasma gondii)[1]
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Dosage:30 mg/kg; 100 mg/kg (twice daily); 100 mg/kg (once daily)
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Administration:p.o.; twice daily; 14 days; p.o.; once daily; 14 days
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Result:Significantly prolonged survival relative to vehicle control in all treatment groups, though all animals eventually succumbed to infection.
Provided significantly better survival in mice treated with 100 mg/kg twice daily compared to those treated with 100 mg/kg once daily.
Showed substantial suppression of parasite burden (reduced bioluminescence signals) and delayed weight loss in mice treated with 100 mg/kg twice daily compared to vehicle control and the 30 mg/kg twice daily group.
Chemical Information
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Molecular Weight 414.34
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Formula C18H13F3N8O
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SMILES
NC1=C2C(OC3=NC=CC(C4=CN=C(N=C4)C(F)(F)F)=C3)=NN(C2=NC=N1)C5CC5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TgCDPK1-IN-1 Related Classifications
HY-184426 Related Classifications
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