5-(N,N-Hexamethylene)-amilorid

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5-(N,N-Hexamethylene)-amiloride

CAS No. : 1428-95-1

MCE 国际站：5-(N,N-Hexamethylene)-amiloride

产品活性：5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride)，是 amiloride 的衍生物，也是一种有效的 Na⁺/H⁺ 交换抑制剂，降低白血病细胞的细胞内 pH (pH_i) 并诱导其凋亡。5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) 也是一种 HIV-1 Vpu 病毒离子通道抑制剂，抑制培养在 L929 细胞中的小鼠肝炎病毒 (MHV) 复制和 HCoV229E 复制，EC₅₀ 值分别为 3.91 μM 和 1.34 μM。

研究领域：Membrane Transporter/Ion Channel  |  Anti-infection  |  Apoptosis

作用靶点：Sodium Channel  |  HIV  |  Apoptosis

In Vitro: 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.

In Vivo: 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 model
Dosage: 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 ratio	Blood CL (mL/min/kg)	Blood Vss (L/kg)
Female Balb/c mice	0.62	86	2.0	1.5	1.5	59	1.4
Sprague Dawley rats	3.2	83.5	5.3	1.6	1.8	46.2	2.9
	% IV dose excreted in urine (0-24 h)	Renal Blood CL (mL/min/kg)	Non-Renal Blood CL (mL/min/kg)
Sprague Dawley rats	0.5	0.2	46.0

Note: B/P means blood-to-plasma partitioning ratio; female Balb/c mice (17-27 g, non-fasted); male Sprague Dawley rats (238-325 g, overnight-fasted).

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