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Art. -Nr.: HY-155103

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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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CAS. Nr.: 2961381-94-0
Formel: C₂₁H₁₉FN₄O₄
Molecular Weight:410.40

Speicherung:

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

Data Sheet (280 KB)

Antitrypanosomal agent 15 Chemical Structure

CAS. Nr.: 2961381-94-0

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
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Beschreibung

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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.

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.

Chemical Information

CAS. Nr. 2961381-94-0
Molecular Weight 410.40
Formel C₂₁H₁₉FN₄O₄
SMILES

CNC(C1=C(F)C=CC(NC(C2=NN(C(C=C2)=O)CC3=CC=C(OC)C=C3)=O)=C1)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Thomas MG, et al. Structure-Guided Design and Synthesis of a Pyridazinone Series of Trypanosoma cruzi Proteasome Inhibitors. J Med Chem. 2023;66(15):10413-10431. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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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Antitrypanosomal agent 15

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Biologische Aktivität

Chemical Information

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Help & FAQs

Antitrypanosomal agent 15 Related Classifications

HY-155103 Related Classifications