午夜插插,噜噜噜影院,啪啪伊人网,欧美熟夫,景甜吻戏视频,男人强操性感蕾丝美女视频在线网站,日本美女跳舞视频

返回ChemicalBook首頁>CAS數(shù)據(jù)庫列表>2609-46-3

2609-46-3

中文名稱 脒氯嗪
英文名稱 AMILORIDE
CAS 2609-46-3
EINECS 編號 220-024-7
分子式 C6H8ClN7O
MDL 編號 MFCD00077316
分子量 229.63
MOL 文件 2609-46-3.mol
2609-46-3 結(jié)構(gòu)式 2609-46-3 結(jié)構(gòu)式

基本信息

中文別名
胍酰吡嗪
脒氯嗪
英文別名
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
所屬類別
分析化學:對照品

物理化學性質(zhì)

熔點240.5-241.5°
密度2.11±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)pKa 8.7 (Uncertain)
形態(tài)Solid
顏色Off-white to light yellow
水溶解性659g/L(25 ºC)
CAS 數(shù)據(jù)庫2609-46-3(CAS DataBase Reference)

常見問題列表

應用

脒氯嗪為阿米洛利生產(chǎn)過程中產(chǎn)生的雜質(zhì)。鹽酸阿米洛利具有良好的保鉀排鈉功能,可選擇性作用于腎小管的細胞內(nèi)膜上,能阻滯鈉進入細胞內(nèi),從而降低細胞腔壁負電勢,使K+,H+排泄受阻而顯示保K+作用。

制備

阿米洛利雜質(zhì)脒氯嗪制備如下:將N-脒基-3,5-二氨基-6-碘-2-吡嗪甲酰胺鹽酸鹽(3.50g,0.01摩爾),氯化亞銅(0.024摩爾)和六甲基磷酰胺(30ml)并在100℃加熱保持15分鐘。冷卻至環(huán)境溫度后,將反應混合物添加至氰化鈉水溶液(100mL)中,在25℃下攪拌1/2小時,并通過抽濾收集固體沉淀物,用水洗滌,然后用氯仿洗滌。將產(chǎn)物溶于沸水(50毫升)中,用6NHCl處理并冷卻,得到1.43克脒氯嗪。

脒氯嗪

生物活性
Amiloride (MK-870) 是上皮鈉通道 (ENaC) 和尿激酶型纖溶酶原激活物受體 (uTPA) 的抑制劑。Amiloride 是 polycystin-2 (PC2; TRPP2) 通道阻斷劑。
靶點

ENaC; uTPA; polycystin-2(TRPP2)

體外研究

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).

體內(nèi)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.

"2609-46-3" 相關(guān)產(chǎn)品信息
290-37-9 2016-88-8 873-83-6