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编 号：F756203
分子式：C20H18ClF2N3O3
分子量：421.83
分子式：C20H18ClF2N3O3
分子量：421.83
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CAS No: 2827061-47-0
产品详情
生物活性：
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).
体内研究：
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.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.Animal Model:NMRI mice, hemolymphatic mice model (Stage I)
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)
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
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)cmpsolubility 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-41279/66311/1191.0/1.617/91700/5635.2/172.3/4.476/128
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.
体外研究：
20S Proteasome-IN-4 (Compound 7) (24 h) inhibits T. b. brucei growth with an EC50 of 20S Proteasome-IN-4 相关抗体:
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).
体内研究：
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.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.Animal Model:NMRI mice, hemolymphatic mice model (Stage I)
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)
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
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)cmpsolubility 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-41279/66311/1191.0/1.617/91700/5635.2/172.3/4.476/128
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.
体外研究：
20S Proteasome-IN-4 (Compound 7) (24 h) inhibits T. b. brucei growth with an EC50 of 20S Proteasome-IN-4 相关抗体:
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