2. Metabolic Enzyme/Protease Anti-infection
  3. Proteasome Parasite
  4. Antitrypanosomal agent 15

Antitrypanosomal agent 15 (compound 26) is an orally active, brain-penetrant, selective inhibitor against Trypanosoma cruzi proteasome, with an pIC50 of 7.4 and <4 for T. cruzi and human proteasome, respectively. Antitrypanosomal agent 15 has favorable ADME properties and can be used for Chagas disease study.

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Antitrypanosomal agent 15 Chemical Structure

Antitrypanosomal agent 15 Chemical Structure

CAS No. : 2961381-94-0

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Antitrypanosomal agent 15 Related Antibodies

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Description

Antitrypanosomal agent 15 (compound 26) is an orally active, brain-penetrant, selective inhibitor against Trypanosoma cruzi proteasome, with an pIC50 of 7.4 and <4 for T. cruzi and human proteasome, respectively. Antitrypanosomal agent 15 has favorable ADME properties and can be used for Chagas disease study[1].

In Vitro

Antitrypanosomal agent 15 (compound 26) has pEC50 of 6.1 and 4.4 against intracellular T. cruzi amastigotes and host VERO cells, and has efflux ratio of 1.8 and FaSSIF (the fasted state simulated intestinal fluid solubility) of 339 μM[1].

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

Antitrypanosomal agent 15 Related Antibodies
In Vivo

Antitrypanosomal agent 15 (compound 26) (50 mg/kg b.i.d for 20 days, p.o.) shows good solubility and permeability, but has no curative towards in chronic mouse model of Chagas disease[1].

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

Animal Model: The chronic mouse model of Chagas disease[1]
Dosage: 50 mg/kg b.i.d for 20days
Administration: Oral gavage (p.o.)
Result: Was not curative .
Was above EC99 for approximately 5 h after the first dose on day 1, but dropped to less than 2 h after the first dose by day 20.
Molecular Weight

410.40

Formula

C21H19FN4O4
CAS No.
SMILES

CNC(C1=C(F)C=CC(NC(C2=NN(C(C=C2)=O)CC3=CC=C(OC)C=C3)=O)=C1)=O
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Antitrypanosomal agent 15 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Antitrypanosomal agent 152961381-94-0Antitrypanosomal agent15Antitrypanosomal agent-15ProteasomeParasiteChagas diseaseTrypanosoma cruziAntiparasiticInhibitorinhibitorinhibit

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