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Cat. No.: 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 No.: 2961381-94-0
Formule: C₂₁H₁₉FN₄O₄
Masse moléculaire:410.40

Stockage:

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

Data Sheet (280 KB)

Antitrypanosomal agent 15 Chemical Structure

CAS No.: 2961381-94-0

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
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Description

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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 No. 2961381-94-0
Masse moléculaire 410.40
Formule C₂₁H₁₉FN₄O₄
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
Instruction de manipulation (2659 KB)

Références

[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]

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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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Pureté et documentation
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Antitrypanosomal agent 15

Voir tous les produits spécifiques à Isoform Parasite

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

Antitrypanosomal agent 15 Related Classifications

HY-155103 Related Classifications