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).
For research use only. We do not sell to patients.
- CAS No.: 2827061-47-0
- Formula: C20H18ClF2N3O3
- Molecular Weight:421.83
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IC50: 6.3 nM (T. b. brucei 20S proteasome)[1]
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.
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.
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Animal Model:NMRI mice, hemolymphatic mice model (Stage I)[1]
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Dosage:3 mg/kg
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Administration:Oral gavage, once a day for 4 days
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Result:Achieved complete cure of the stage I infection.
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Animal Model:CD1 mice, meningoncephalic mice model (stage II)[1]
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Dosage:15 mg/kg
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Administration:Oral gavage, twice a day for 1 week
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Result:Achieved complete cure of the stage II infection.
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Animal Model:BALB/c mice and Wistar rats[1]
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Dosage:1 mg/kg or 3 mg/kg
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Administration:Intravenous or oral administration (Pharmacokinetic Analysis)
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Result:ADME and PK Data for 20S Proteasome-IN-4 (Compound 7)[1]
cmp solubility pH 6.8 μM LM CLint (m/r) [μL/min/mg] LM scaled CLint [mL/min/kg] (m/r) fu plasma [%] (m/r) CLp [mL/min/kg] (m/r) CLu [mL/min/kg] (m/r) AUCPO [μM•h] (m/r) AUCIV [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; fu,plasma from PPB; LM scaled Clint = (LM Clint•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: Clp = Clu/fu, with Clp observed clearance. Mouse and rat PK 1 mpk IV/3 mpk PO.
Chemical Information
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CAS No. 2827061-47-0
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Molecular Weight 421.83
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Formula C20H18ClF2N3O3
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SMILES
ClC1=CC=C2C(C(NC3=CC=CC(F)=C3F)=CC(C(NC[C@H](CO)OC)=O)=N2)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
20S Proteasome-IN-4 Related Classifications
HY-151195 Related Classifications
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