4-(N-(tert-butyl)acetamido)-5-(diallylamino)-3-(pentan-3-yloxy)cyclohex-1-enecarboxylate;(3R,4S,5R)-ethyl 4-acetamido-5-amino-3-(pentan-3-yloxy)cyclohex-1-enecarboxylate;ethyl (3R,4S,5R)-4-acetamido-5-amino-3-(pentan-3-yloxy)cyclohex-1-ene-1-carboxylate;ethyl(3S,4S,5R)-4-acetamido-5-amino-3-(1-ethylpropoxy)-cyclohex-1-ene-1-carboxylate;1-Cyclohexene-1-carboxylic acid, 4-(acetylamino)-5-amino-3-(1-ethylpropoxy)-, ethyl ester, (3R,4S,5R)-;(3R,4S,5R)-ethyl4-acetamido-5-amino-3-(pentan-3-yloxy)cyclohex-1-enecarboxylatehydrochloride;Oseltamivir Impurity 27Q: What is
Oseltamivir Impurity 27 Q: What is the CAS Number of
Oseltamivir Impurity 27
Cas No.
1373232-26-8
分子式
C16H28N2O4
分子量
312.40
包装储存
-20°C
生物活性
Cl-amidine hydrochloride 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 hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model[1][2][3][4][5].
Cl-amidine (75 mg/kg,每天一次,腹腔注射) 抑制和处理 DSS 诱导的小鼠结肠炎[2]。
Cl-amidine (5、25、75 mg/kg,口服强饲法,每天一次) 导致组织学评分显著降低,且呈剂量依赖性[2]。
Animal Model: C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)[2].
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)[2].
Dosage: 5, 25, 75 mg/kg.
Administration: Oral gavage once daily.
Result: Led to significant reductions in the histology scores.
[1]. Yuan Luo, et al. Inhibitors and Inactivators of Protein Arginine Deiminase 4: Functional and Structural Characterization. Biochemistry. 2006 Oct 3; 45(39): 11727–11736.
[2]. Chumanevich AA, et al. Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine deiminase inhibitor. Am J Physiol Gastrointest Liver Physiol. 2011 Jun;300(6):G929-38.
[3]. Witalison EE, et al. Molecular targeting of protein arginine deiminases to suppress colitis and prevent colon cancer. Oncotarget. 2015 Nov 3;6(34):36053-62.
[4]. Biron BM, et al., Cl-Amidine Prevents Histone 3 Citrullination and Neutrophil Extracellular Trap Formation, and Improves Survival in a Murine Sepsis Model. J Innate Immun. 2017;9(1):22-32.