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- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Benzamil Hydrochloride Hydrate
- 库存：
999
- 供应商：
北京索莱宝科技有限公司
- CAS号：
161804-20-2
- 规格：
10mg/5mg/50mg/100mg
| 规格： | 10mg | 产品价格： | ¥650.00 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ¥490.00 |
| 规格： | 50mg | 产品价格： | ¥2590.00 |
| 规格： | 100mg | 产品价格： | ¥4590.00 |
| CAS | 161804-20-2 |
| 英文名称 | Benzamil Hydrochloride Hydrate |
| 别名 | Benzylamiloridehydrochloride |
| 分子式 | C13H14ClN7O·HCl·xH2O |
| 分子量 | 356.21 (as Anhydrous) |
| 规格 | 10mg ; 5mg ; 50mg ; 100mg |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | Light yellow to yellow Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 | 冷藏运输 |
| EC | 634-062-0 |
| MDL | MFCD00069219 |
| SMILES | O=C(C1=NC(Cl)=C(N)N=C1N)NC(NCC2=CC=CC=C2)=N.[H]Cl |
| InChIKey | ZNWMRWWNJBXNKJ-UHFFFAOYSA-N |
| InChI | InChI=1S/C13H14ClN7O.ClH/c14-9-11(16)20-10(15)8(19-9)12(22)21-13(17)18-6-7-4-2-1-3-5-7;/h1-5H，6H2，(H4，15，16，20)(H3，17，18，21，22);1H |
| PubChem CID | 5702295 |
| 靶点 | Sodium Channel |
| 通路 | Membrane Transporter&Ion Channel |
| 背景说明 | Benzamil hydrochloride 是钠通道(ENaC)的特异性阻断剂。 |
| 生物活性 | Benzamil hydrochloride (Benzylamiloride hydrochloride)， an Amiloride analogue， is a Na+/Ca2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker， and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca2+-activated currents， with an IC50 of 1.1 μM.[1-5] |
| In Vitro | Benzamil hydrochloride (Benzylamiloride hydrochloride) 抑制神经元和异源表达的小电导 Ca2+-激活的 K2+ 通道[4]。 |
| In Vivo | Benzamil hydrochloride (Benzylamiloride hydrochloride) (0.7 mg/kg/天；sc) 处理的中风倾向自发性高血压大鼠 (SHRSP) 在 SHRSP 大鼠中平均存活至 16.1 周龄[5]。 |
| 细胞实验 | Individual CCD segments are dissected from rabbit and mouse kidney.The measurements of [Na+]i are used as a reflection of Na+ transport across the apical membrane. EnaC-specific activity is assessed by applying 10?6 M of the ENaC blocker Benzamil hydrochloride， a concentration that does not affect Na+:H+ exchange. Experiments are performed in the presence/absence of luminal Benzamil hydrochloride or the Na:H exchanger blocker HOE694 administers with/without the AT1 receptor blocker candesartan. Final DMSO concentrations are below 0.1% [2]. |
| 动物实验 | For the acute intracerebroventricular injection in anesthetized rats. A guide cannula is inserted into the right lateral cerebral ventricle， and Benzamil hydrochloride (0.1 nmol/kg， n=6; 1 nmol/kg， n=6; 10 nmol/kg，n=7) or vehicle (n=6) is injected into the right lateral ventricle through a cannula connected to a microsyringe 15 min before the start of intracerebroventricular infusion of hypertonic NaCl. Each injection consists of a volume of 10 μL deliver manually over a period of 30 s. To investigate the effects of Benzamil hydrochloride on the pressor response induced by intracerebroventricular injection of the pressor agent other than hypertonic NaCl， endothelin-1， which has a potent pressor action in the brain of rats， is intracerebroventricularly injected (1 nmol/10 μL) 15 min after the intracerebroventricular preinjection of Benzamil hydrochloride (10 nmol/kg， n=6) or the vehicle (n=6)， and mean arterial pressure， heart rate， and abdominal sympathetic nerve firings are recorded for 20 min. Catheters are implanted into both the femoral artery and vein of 12-wk-old male rats anesthetized with urethan. Both catheters are filled with heparinized saline (50 U/mL). Fifteen minutes before the start of intracerebroventricular infusion of hypertonic NaCl， Benzamil hydrochloride (10 nmol/kg， n=6) or vehicle (10 μL， n=6) is injected into a tube connects to the femoral venous catheter by directly inserting the microsyringe， and 0.1 ml of isotonic saline solution is injected through the catheter to deliver the contents into the venous circulation[1]. |
| 数据来源文献 | [1]. Fischer KG， et al. Characterization of a Na(+)-Ca(2+) exchanger in podocytes. Nephrol Dial Transplant. 2002 Oct;17(10):1742-50. [2]. Wang X， et al. Effects of amiloride， benzamil， and alterations in extracellular Na+ on the rat afferent arteriole and its myogenic response. Am J Physiol Renal Physiol. 2008 Jul;295(1):F272-82. [3]. Dai XQ， et al. Inhibition of TRPP3 channel by amiloride and analogs. Mol Pharmacol. 2007 Dec;72(6):1576-85. [4]. Casta?eda MS， et al. Benzamil inhibits neuronal and heterologously expressed small conductance Ca2+-activated K+channels. Neuropharmacology. 2019 Nov 1;158:107738. [5]. Teiwes J， et al. Epithelial sodium channel inhibition in cardiovascular disease. A potential role for amiloride. Am J Hypertens. 2007 Jan;20(1):109-17. |
| 单位 | 瓶 |
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文献和实验Synthesis of Peptidomimetic Conjugates of Cyclic Nucleoside Phosphonates
ester hydrochloride (Aldrich) Ethan‐1,2‐diol (ethylene glycol) 1‐Hydroxybenzotriazole hydrate (HOBt; Aldrich
acedapsone beclomethasone acenocumarol bemegride acetarsol benactyzine hydrochloride acetazolamide bendroflumethiazide acetylcholine
; distilled over CaH 2 ) Propargylamine N ‐Hydroxybenzotriazole hydrate (HOBt
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