5-(N,N-Hexamethylene)-amiloride|1428-95-1|(Hexamethylene amiloride; HMA)-陌孚医药/Medlife

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

目录号: PL11393 纯度: ≥98%

CAS No. :1428-95-1

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中文名称	5-(N,N-Hexamethylene)-amiloride
中文别名	阿米洛利;5-(N,N-己基亚甲基)-阿米洛利;阿米洛利溶液,100PPM
英文名称	5-(N,N-Hexamethylene)-amiloride
英文别名	amiloride;3-amino-5-(azepan-1-yl)-6-chloro-N-(diaminomethylidene)pyrazine-2-carboxamide;5-(N,N-HEXAMETHYLENE)-AMILORIDE;3-amino-5-azepan-1-yl-6-chloro-pyrazine-2-carboxylic acid carbamimidoylamide;Hexamethyleneamiloride;HMA;HMA-5;amipromizide;AMILORIDE,5-(N,N-HEXAMETHYLENE)-;HMA (5-(N,N-Hexamethylene)amiloride);5-(N,N-Hexamethylene)amiloride Solution, 100ppm;3-amino-5-(azepan-1-yl)-6-chloro-N-(diaminomethylene)pyrazinamide;H+ ANTIPORTER INH;AMILORIDE, 5-(N,N-HEXAMETHYLENE) >93% NA +/H+ ANTIPORTER INH;5-(N,N-Hexamethylene)-amiloride
Cas No.	1428-95-1
分子式	C₁₂H₁₈ClN₇O
分子量	311.77
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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 EC 50 s of 3.91 μM and 1.34 μM, respectively.
性状	Solid
IC50 & Target[1][2]	HIV-1
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
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)
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
参考文献	[1]. 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. [2]. 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.

溶解度数据	In Vitro: DMSO : 100 mg/mL (320.75 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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