5-(N,N-Hexamethylene)-amiloride Hexamethylene amiloride; HMA|cas:1428-95-1|西域试剂

5-(N,N-Hexamethylene)-amiloride Hexamethylene amiloride; HMA,98.42%

产品编号：Bellancom-128067| CAS NO：1428-95-1| 分子式：C₁₂H₁₈ClN₇O| 分子量：311.77

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 (pHi) 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) 复制和人冠状病毒 229E (HCoV229E) 复制，EC50 值分别为 3.91 μM 和 1.34 μM。

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货号	价格	库存与货期
Bellancom-128067	￥1000.00	杭州北京（现货）
Bellancom-128067	￥1600.00	杭州北京（现货）
Bellancom-128067	￥3500.00	杭州北京（现货）

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5-(N,N-Hexamethylene)-amiloride Hexamethylene amiloride; HMA

产品介绍

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。

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 (pH_i) 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:

In vitro pharmacokinetics properties

Concentration:

1 μM

Incubation Time:

0-60 min

Result:

	t_1/2 (min)	CL_int (μL/min/mg protein)	CL_int (μL/min/mg protein)
Human liver microsomers in vitro	73	24	74
Mouse liver microsomers in vitro	2.4	726	2243

体内研究
(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/kg Administration: Intravenous injection; single does; collected 10 min and 60 min after treatment.

	t_1/2 (h)	Plasma CL_int (mL/min/kg)	Plasma V_ss (L/kg)	Plasma AUC_0-inf (h·μM)	B/P ratio	Blood CL (mL/min/kg)	Blood V_ss (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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

	t_1/2 (h)	Plasma CL_int (mL/min/kg)	Plasma V_ss (L/kg)	Plasma AUC_0-inf (h·μM)	B/P ratio	Blood CL (mL/min/kg)	Blood V_ss (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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

	t_1/2 (h)	Plasma CL_int (mL/min/kg)	Plasma V_ss (L/kg)	Plasma AUC_0-inf (h·μM)	B/P ratio	Blood CL (mL/min/kg)	Blood V_ss (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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (320.75 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2075 mL	16.0375 mL	32.0749 mL
5 mM	0.6415 mL	3.2075 mL	6.4150 mL
10 mM	0.3207 mL	1.6037 mL	3.2075 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.08 mg/mL (6.67 mM); Clear solution; Need ultrasonic

此方案可获得 2.08 mg/mL (6.67 mM) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (6.67 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.67 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.67 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.67 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在西域网站选购。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

. Rich IN, et al. Apoptosis of leukemic cells accompanies reduction in intracellular pH after targeted inhibition of the Na(+)/H(+) exchanger. Blood. 2000 Feb 15;95(4):1427-34. [Content Brief]

. Wilson L, et al. Hexamethylene amiloride blocks E protein ion channels and inhibits coronavirus replication. Virology. 2006 Sep 30;353(2):294-306. Epub 2006 Jul 3. [Content Brief]

. Buckley BJ, et al. Systematic evaluation of structure-property relationships and pharmacokinetics in 6-(hetero)aryl-substituted matched pair analogs of amiloride and 5-(N,N-hexamethylene)amiloride. Bioorg Med Chem. 2021 May 1;37:116116. [Content Brief]

化学品安全说明书(MSDS)

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质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

符号	GHS06
信号词	Danger
危害声明	H301-H311-H331
警示性声明	P261-P280-P301 + P310-P311
个人防护装备	Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges
危害码 (欧洲)	T
风险声明 (欧洲)	23/24/25
安全声明 (欧洲)	22-36/37/39-45
危险品运输编码	UN 2811
WGK德国	3
包装等级	III
危险类别	6.1(b)
海关编码	2934999090

5-(N,N-Hexamethylene)-amiloride Hexamethylene amiloride; HMA,98.42%

5-(N,N-Hexamethylene)-amiloride Hexamethylene amiloride; HMA

化学品安全说明书(MSDS)

质检证书(COA)

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