Cl-amidine hydrochloride

Research use only, not for human use.

Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor (IC50: 5.9 μM for PAD4).

Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor (IC50: 5.9 μM for PAD4). Cl-amidine hydrochloride induces apoptosis in cancer cells and it also induces microRNA (miR)-16 in vitro causing cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation. It improves survival in a murine sepsis model.

Apoptosis Analysis.Cell Line:TK6 lymphoblastoid cells and HT29 colon cancer cells. Concentration:0, 5, 10, 15, 20, 25, 50 μg/mL.Incubation Time:24 h.Result:Induced apoptosis 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.

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Apoptosis

Apoptosis

Apoptosis|MicroRNA|PAD4

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1373232-26-8

347.24

C14H20Cl2N4O2

>98% (HPLC)

H2O:50 mg/mL (143.99 mM; Need ultrasonic);DMSO:19.23 mg/mL (55.38 mM; Need ultrasonic)

O=C(N[C@H](C(N)=O)CCCNC(CCl)=N)C1=CC=CC=C1.[H]Cl

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(-20℃)

With Ice Pack

≥ 2 years