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Art. -Nr.: HY-151195

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20S Proteasome-IN-4

20S Proteasome-IN-4 (Compound 7) is a brain-penetrant, parasite-selective, orally active 20S proteasome inhibitor with an IC₅₀ of 6.3 nM against T. b. brucei 20S proteasome. 20S Proteasome-IN-4 can be used for the research of human African trypanosomiasis (HAT).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2827061-47-0
Formel: C₂₀H₁₈ClF₂N₃O₃
Molecular Weight:421.83

Speicherung:

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

Data Sheet (274 KB)

20S Proteasome-IN-4 Chemical Structure

CAS. Nr.: 2827061-47-0

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC₅₀: 6.3 nM (T. b. brucei 20S proteasome)^[1]

Alle Parasite Isoform-spezifische Produkte anzeigen :

In Vitro

20S Proteasome-IN-4 (Compound 7) (24 h) inhibits T. b. brucei growth with an EC₅₀ of <2.5 nM^[1].

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

In Vivo

20S Proteasome-IN-4 (Compound 7) (3 mg/kg; i.g.; once a day for 4 days) cures a stage I mouse model of human African trypanosomiasis^[1].
20S Proteasome-IN-4 (15 mg/kg; i.g.; twice a day for 1 week) cures a stage II mouse model of human African trypanosomiasis^[1].

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

Animal Model:

NMRI mice, hemolymphatic mice model (Stage I)^[1]
Dosage:

3 mg/kg
Administration:

Oral gavage, once a day for 4 days
Result:

Achieved complete cure of the stage I infection.

Animal Model:

CD1 mice, meningoncephalic mice model (stage II)^[1]
Dosage:

15 mg/kg
Administration:

Oral gavage, twice a day for 1 week
Result:

Achieved complete cure of the stage II infection.

Animal Model:

BALB/c mice and Wistar rats^[1]
Dosage:

1 mg/kg or 3 mg/kg
Administration:

Intravenous or oral administration (Pharmacokinetic Analysis)

Result:

ADME and PK Data for 20S Proteasome-IN-4 (Compound 7)^[1]

cmp	solubility pH 6.8 μM	LM CL_int (m/r) [μL/min/mg]	LM scaled CL_int [mL/min/kg] (m/r)	f_u plasma [%] (m/r)	CL_p [mL/min/kg] (m/r)	CL_u [mL/min/kg] (m/r)	AUC_PO [μM•h] (m/r)	AUC_IV [μM•h] (m/r)	%F m/r
20S Proteasome-IN-4	12	79/66	311/119	1.0/1.6	17/9	1700/563	5.2/17	2.3/4.4	76/128

Solubility: Miniaturized shake flask solubility in phosphate buffer; f_u,plasma from PPB; LM scaled Cl_int = (LM Cl_int•SF1•SF2)/1000 with SF1 (mg protein per g liver) m,r = 45, SF2 (g liver per kg BW); m = 87.5, SF2 r = 40. Unbound clearance: Cl_p = Cl_u/f_u, with Cl_p observed clearance. Mouse and rat PK 1 mpk IV/3 mpk PO.

Chemical Information

CAS. Nr. 2827061-47-0
Molecular Weight 421.83
Formel C₂₀H₁₈ClF₂N₃O₃
SMILES

ClC1=CC=C2C(C(NC3=CC=CC(F)=C3F)=CC(C(NC[C@H](CO)OC)=O)=N2)=C1
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 (274 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]. Koester DC, et al. Discovery of Novel Quinoline-Based Proteasome Inhibitors for Human African Trypanosomiasis (HAT). J Med Chem. 2022 Aug 22. [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.

Keywords

MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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20S Proteasome-IN-4

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

20S Proteasome-IN-4 Related Classifications

HY-151195 Related Classifications