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Cat. No.: HY-184426

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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 TgCDPK^G128M. 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

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

TgCDPK1-IN-1 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All Parasite Isoforms :

In Vitro

Anti-cancerParasitic InfectionOthers

Anti-cancer

TgCDPK1-IN-1 (20 μM) induces 8.6% cytotoxicity in HepG2 cells^[1].

Parasitic Infection

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].

Others

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 TgCDPK1^G128M mutant by 13.6%^[1].

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

Parmacokinetics

Species	Dose	Route	AUC_0-24	T_1/2	C_max	CL	V_d
Mice^[1]	10 mg/kg	p.o.	12245 ng·h/mL	2.5 h	/	/	/
Mice^[1]	3 mg/kg	i.v.	/	/	1959 ng/mL	29.6 mL/min/kg	2.8 L/kg

In Vivo

Parasitic Infection

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].
TgCDPK1-IN-1 (30-100 mg/kg; p.o.; 1-2 times daily) cures acute toxoplasmosis in immunocompetent C57BL/6 mice at the dose of 100 mg/kg p.o. once daily, resulting in 100% survival rate with no signs of chronic infection; it achieves partial control at the dose of 30 mg/kg p.o. twice daily, with 100% mouse survival rate but persistent chronic infection^[1].

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

Animal Model:

C57BL/6 mice (immunocompetent; infected via i.p. injection with ME49-FLUC Toxoplasma gondii)^[1]
Dosage:

30 mg/kg; 100 mg/kg
Administration:

p.o.; twice daily; p.o.; once daily
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.

Animal Model:

Ifngr1−/− mice (immunocompromised; infected via oral gavage with 5 tissue cysts of ME49-FLUC Toxoplasma gondii)^[1]
Dosage:

30 mg/kg; 100 mg/kg (twice daily); 100 mg/kg (once daily)
Administration:

p.o.; twice daily; 14 days; p.o.; once daily; 14 days
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

Molecular Weight 414.34
Formula C₁₈H₁₃F₃N₈O
SMILES

NC1=C2C(OC3=NC=CC(C4=CN=C(N=C4)C(F)(F)F)=C3)=NN(C2=NC=N1)C5CC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Mannino MP, et al. Lead Optimization of TgCDPK1 Inhibitors for the Treatment of Toxoplasmosis. Journal of medicinal chemistry. 2026 Jun 25;69(12):14365-14389. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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