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编 号：F548199
分子式：C16H20ClF3N4O4
分子量：424.8
分子式：C16H20ClF3N4O4
分子量：424.8
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CAS No: 1043444-18-3
产品详情
生物活性：
Cl-amidine TFA is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine TFA induces apoptosis in cancer cells. Cl-amidine TFA induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine TFA prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.
体内研究：
Cl-amidine (75 mg/kg, ip once daily) suppresses and treats DSS-induced colitis in mice.Cl-amidine (5, 25, 75 mg/kg, oral gavage, once daily) leads to significant reductions in the histology scores dose-dependently.Animal Model:C57BL/6 mice (8-12 wk old, DSS mouse model of colitis).
Dosage:75 mg/kg.
Administration:IP once daily.
Result:Suppressed PAD activity, protein citrullination, and PAD levels in the colon in vivo.
Animal Model:C57BL/6 mice (8-12 wk old, DSS mouse model of colitis).
Dosage:5, 25, 75 mg/kg.
Administration:Oral gavage once daily.
Result:Led to significant reductions in the histology scores.
体外研究：
Cl-amidine is a bioavailable haloacetamidine-based compound that inhibits all the active PAD isozymes with near equal potency (kinact/KI=13,000 M-1?min-1 for PAD4). Cl-amidine (0, 5, 10, 15, 20, 25, 50 μg/mL, 24 hours) induces apoptosis in TK6 lymphoblastoid cells and HT29 colon cancer cells in a dose-dependent manner. Interestingly, the colon cancer cell line (HT29) is relatively resistant to apoptosis caused by Cl-amidine.Cl-amidine irreversibly inactivates PADs by covalently modifying an active site cysteine that is important for its catalytic activity.
Cl-amidine TFA is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine TFA induces apoptosis in cancer cells. Cl-amidine TFA induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine TFA prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.
体内研究：
Cl-amidine (75 mg/kg, ip once daily) suppresses and treats DSS-induced colitis in mice.Cl-amidine (5, 25, 75 mg/kg, oral gavage, once daily) leads to significant reductions in the histology scores dose-dependently.Animal Model:C57BL/6 mice (8-12 wk old, DSS mouse model of colitis).
Dosage:75 mg/kg.
Administration:IP once daily.
Result:Suppressed PAD activity, protein citrullination, and PAD levels in the colon in vivo.
Animal Model:C57BL/6 mice (8-12 wk old, DSS mouse model of colitis).
Dosage:5, 25, 75 mg/kg.
Administration:Oral gavage once daily.
Result:Led to significant reductions in the histology scores.
体外研究：
Cl-amidine is a bioavailable haloacetamidine-based compound that inhibits all the active PAD isozymes with near equal potency (kinact/KI=13,000 M-1?min-1 for PAD4). Cl-amidine (0, 5, 10, 15, 20, 25, 50 μg/mL, 24 hours) induces apoptosis in TK6 lymphoblastoid cells and HT29 colon cancer cells in a dose-dependent manner. Interestingly, the colon cancer cell line (HT29) is relatively resistant to apoptosis caused by Cl-amidine.Cl-amidine irreversibly inactivates PADs by covalently modifying an active site cysteine that is important for its catalytic activity.
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