产品
编 号：F160598
分子式：C12H18ClN7O
分子量：311.77
分子式：C12H18ClN7O
分子量：311.77
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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询价
5mg
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10mg
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询价
50mg
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100mg
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结构图
CAS No: 1428-95-1
产品详情
生物活性：
5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively.
体内研究：
5-(N,N-Hexamethylene)-amiloride (2.5 mg/kg; i.v.; single dose) shows short half-life and lowly oral bioavailability of 4.5%.In vivo pharmacokinetics in mice or rat modelDosage: 2.5 mg/kgAdministration: Intravenous injection; single does; collected 10 min and 60 min after treatment.t1/2 (h)Plasma CLint (mL/min/kg)Plasma Vss (L/kg)Plasma AUC0-inf (h·μM)B/P ratioBlood CL (mL/min/kg)Blood Vss (L/kg)
Female Balb/c mice0.62862.01.51.5591.4
Sprague Dawley rats3.283.55.31.61.846.22.9
% IV dose excreted in urine (0-24 h)Renal Blood CL (mL/min/kg)Non-Renal Blood CL (mL/min/kg)
Sprague Dawley rats0.50.246.0
Note: B/P means blood-to-plasma partitioning ratio; female Balb/c mice (17-27 g, non-fasted); male SpragueDawley rats (238-325 g, overnight-fasted).
体外研究：
5-(N,N-Hexamethylene)-amiloride inhibits human cardiac ion channels hERG (in CHO cells), Nav1.5 and Cav1.2 (in EHK293 cells) with of 3.3 μM, 30 μM, 8.3 μM, respectively, inelectrophysiology assays.5-(N,N-Hexamethylene)-amiloride (1 μM; 0-60 min; 37 ℃) exhibits microsomal stability, (1 μg/mL; 4.2 h; 37 ℃) shows mouse plasma stability and plasma protein binding, (20 μM; 4 h) displays Caco-2 cell permeability, cardiac ion channel activity.
5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively.
体内研究：
5-(N,N-Hexamethylene)-amiloride (2.5 mg/kg; i.v.; single dose) shows short half-life and lowly oral bioavailability of 4.5%.In vivo pharmacokinetics in mice or rat modelDosage: 2.5 mg/kgAdministration: Intravenous injection; single does; collected 10 min and 60 min after treatment.t1/2 (h)Plasma CLint (mL/min/kg)Plasma Vss (L/kg)Plasma AUC0-inf (h·μM)B/P ratioBlood CL (mL/min/kg)Blood Vss (L/kg)
Female Balb/c mice0.62862.01.51.5591.4
Sprague Dawley rats3.283.55.31.61.846.22.9
% IV dose excreted in urine (0-24 h)Renal Blood CL (mL/min/kg)Non-Renal Blood CL (mL/min/kg)
Sprague Dawley rats0.50.246.0
Note: B/P means blood-to-plasma partitioning ratio; female Balb/c mice (17-27 g, non-fasted); male SpragueDawley rats (238-325 g, overnight-fasted).
体外研究：
5-(N,N-Hexamethylene)-amiloride inhibits human cardiac ion channels hERG (in CHO cells), Nav1.5 and Cav1.2 (in EHK293 cells) with of 3.3 μM, 30 μM, 8.3 μM, respectively, inelectrophysiology assays.5-(N,N-Hexamethylene)-amiloride (1 μM; 0-60 min; 37 ℃) exhibits microsomal stability, (1 μg/mL; 4.2 h; 37 ℃) shows mouse plasma stability and plasma protein binding, (20 μM; 4 h) displays Caco-2 cell permeability, cardiac ion channel activity.
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