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
- Purity & Documentation
- References
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Biological Activity
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.
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.
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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