基本信息 物理化学性质 安全数据 常见问题列表 供应商 相关产品
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2609-46-3

中文名称 脒氯嗪
英文名称 AMILORIDE
CAS 2609-46-3
EINECS 编号 220-024-7
分子式 C6H8ClN7O
MDL 编号 MFCD00077316
分子量 229.63
MOL 文件 2609-46-3.mol
结构式 2609-46-3 结构式

基本信息

中文别名 胍酰吡嗪
脒氯嗪
英文别名 AMILORIDE
N-amidino-3,5-diamino-6-chloropyrazine-2-carboxamide
3,5-Diamino-6-chloro-N-(aminoiminomethyl)-2-pyrazinecarboxamide
3,5-Diamino-6-chloro-N-(diaminomethylene)pyrazinecarboxamide
MK-870
所属类别 分析化学:对照品

物理化学性质

熔点 240.5-241.5°
密度 2.11±0.1 g/cm3(Predicted)
储存条件 -20°C储存
溶解度 溶于二甲基亚砜
酸度系数(pKa) pKa 8.7 (Uncertain)
水溶解性 659g/L(25 ºC)
CAS 数据库 2609-46-3(CAS DataBase Reference)

安全数据

危险性符号(GHS)
GHS06
警示词 危险
危险性描述 H319-H300-H315-H412
防范说明 P264-P280-P302+P352-P321-P332+P313-P362-P264-P280-P305+P351+P338-P337+P313P-P264-P270-P301+P310-P321-P330-P405-P501-P273-P501

常见问题列表

应用

脒氯嗪为阿米洛利生产过程中产生的杂质。盐酸阿米洛利具有良好的保钾排钠功能,可选择性作用于肾小管的细胞内膜上,能阻滞钠进入细胞内,从而降低细胞腔壁负电势,使K+,H+排泄受阻而显示保K+作用。

制备

阿米洛利杂质脒氯嗪制备如下:将N-脒基-3,5-二氨基-6-碘-2-吡嗪甲酰胺盐酸盐(3.50g,0.01摩尔),氯化亚铜(0.024摩尔)和六甲基磷酰胺(30ml)并在100℃加热保持15分钟。冷却至环境温度后,将反应混合物添加至氰化钠水溶液(100mL)中,在25℃下搅拌1/2小时,并通过抽滤收集固体沉淀物,用水洗涤,然后用氯仿洗涤。将产物溶于沸水(50毫升)中,用6NHCl处理并冷却,得到1.43克脒氯嗪。

脒氯嗪

生物活性
Amiloride (MK-870) 是上皮钠通道 (ENaC) 和尿激酶型纤溶酶原激活物受体 (uTPA) 的抑制剂。Amiloride 是 polycystin-2 (PC2; TRPP2) 通道阻断剂。
靶点

ENaC; uTPA; polycystin-2(TRPP2)

体外研究

Amiloride blocks δβγ channels with an IC 50 of 2.6 μM (58, 71, 75, 134, 148). The K i of amiloride for δβγ ENaC is 26-fold that of αβγ channels (0.1 μM for αβγ ENaC). Amiloride blockade of δβγ ENaC is much more voltage dependent compared with the αβγ channel. The K i of amiloride for δαβγ channels is 920 and 13.7 μM at -120 and +80 mV, respectively, which significantly differs from that of both αβγ and δβγ channels. Amiloride is a relatively selective inhibitor of the epithelial sodium channel (ENaC) with an IC 50 (the concentration required to reach 50% inhibition of an ion channel) in the concentration range of 0.1 to 0.5 μM. Amiloride is a relatively poor inhibitor of the the Na + /H + exchanger (NHE) with an IC 50 as low as 3 μM in the presence of a low external [Na + ] but as high as 1 mM in the presence of a high [Na + ]. Amiloride is an even weaker inhibitor of the Na + /Ca 2+ exchanger (NCX), with an IC 50 of 1 mM. Amiloride (1 μM) and submicromolar doses of Benzamil (30 nM), doses known to inhibit the ENaC, inhibit the myogenic vasoconstriction response to increasing perfusion pressure by blocking the activity of ENaC proteins. Amiloride completely inhibits Na + influx in doses known to be relatively specific for ENaC (1.5 μM) in vascular smooth muscle cells (VSMC).

体内研究

Amiloride (1 mg/kg/day) subcutaneously is found to reverse the initial increases in collagen deposition and prevent any further increases in the DOCA-salt hypertensive rat. Amiloride delays the onset of proteinuria and improved brain and kidney histologic scores in the saline-drinking, stroke-prone spontaneously hypertensive rats (SHRSP) compared with controls. Amiloride antagonizes or prevents actions of aldosterone in these cells and in cardiovascular and renal tissues in animals with salt-dependent forms of hypertension.

供应商信息 更多

北京百灵威科技有限公司
联系电话: 010-82848833 400-666-7788
产品介绍:
中文名称:脒氯嗪
英文名称:AMiloride hydrochloride
CAS:2609-46-3
包装信息:100Mg
备注:化学试剂、精细化学品、医药中间体、材料中间体
Sigma-Aldrich西格玛奥德里奇(上海)贸易有限公司
联系电话: 021-61415566 800-8193336
产品介绍:
英文名称:Amiloride
CAS:2609-46-3
纯度:>= 98 % HPLC, powder
包装信息:1g, 5g, 10g
备注:A7410
上海安谱实验科技股份有限公司
联系电话: 18501792038
产品介绍:
中文名称:阿米洛利
英文名称:Amiloride
CAS:2609-46-3
纯度:10mg
包装信息:10mg
备注:CDAA-3110190-10mg
湖北诺纳科技有限公司
联系电话: 027-027-59209883 17386169806
产品介绍:
中文名称:脒氯嗪 阿米洛利杂质
CAS:2609-46-3
纯度:98%
包装信息:5ASSAYS/10
湖北云镁科技有限公司
联系电话: 027-59206672 18327059871
产品介绍:
中文名称:脒氯嗪 阿米洛利杂质
CAS:2609-46-3
纯度:99% HPLC
包装信息:5KG;1KG
上海优宁维生物科技股份有限公司
联系电话: 18768175414
产品介绍:
英文名称:Amiloride
包装信息:1g
备注: 见优宁维官网
深圳市华信医药科技有限公司
联系电话: 15671363360
产品介绍:
中文名称:阿米洛利杂质
英文名称:AMILORIDE Impurity
CAS:2609-46-3
纯度:>95% HPLC
包装信息:10mg;20mg;50mg;100mg
备注:详情联系TEL:133-9286-8572,另更多原研参比制剂优势供应中

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