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Amiloride HCl dihydrate/盐酸阿米洛利二水合物 {[allProObj[0].p_purity_real_show]}

货号:A105627 同义名: MK-870 hydrochloride dihydrate; Amiloride hydrochloride dihydrate

Amiloride HCl blocks epithelial sodium channel (ENaC) and is used to treat hypertension and congestive heart failure.

Amiloride HCl dihydrate/盐酸阿米洛利二水合物 化学结构 CAS号:17440-83-4
Amiloride HCl dihydrate/盐酸阿米洛利二水合物 化学结构
CAS号:17440-83-4
Amiloride HCl dihydrate/盐酸阿米洛利二水合物 3D分子结构
CAS号:17440-83-4
Amiloride HCl dihydrate/盐酸阿米洛利二水合物 化学结构 CAS号:17440-83-4
Amiloride HCl dihydrate/盐酸阿米洛利二水合物 3D分子结构 CAS号:17440-83-4
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Amiloride HCl dihydrate/盐酸阿米洛利二水合物 纯度/质量文件 产品仅供科研

货号:A105627 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Sodium Channel 其他靶点 纯度
Tolperisone HCl 99%
Triamterene +++

ENaC, IC50: 4.5 μM

98%
Lamotrigine 98%
Vinpocetine 98%
Zonisamide 99%
Dronedarone HCl 95%
Procainamide HCl 99%
Bupivacaine HCl 99+%
Benzocaine 98%
Carbamazepine ++

Sodium channel, IC50: 131 μM

98%
Quinidine sulfate dihydrate 98%
Ibutilide fumarate 99%+
Dibucaine HCl 99+%
Mexiletine HCl 99%
Phenytoin 99+%
Camostat Mesylate +++

epithelial sodium channel (ENaC), IC50: 50 nM

99%+
Levobupivacaine 97+%
Oxcarbazepine +

sodium channel, IC50: 160 μM

98%
Amiloride HCl dihydrate 97%
Ambroxol 98+%
Primidone 99%
Propafenone 99%
A-803467 ++++

Na(V1.8) channel, IC50: 8 nM

99%+
Rufinamide 99%
Phenytoin sodium 98%
Proparacaine HCl +

Voltage-gated sodium channel, ED50: 3.4 mM

98+%
Amiloride HCl 98%
Riluzole 97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Amiloride HCl dihydrate/盐酸阿米洛利二水合物 生物活性

靶点
  • Sodium Channel

描述 Amiloride is a potent epithelial sodium channel (ENaC) blocker, used in the management of hypertension and congestive heart failure. It works as both a selective T-type calcium channel/epithelial sodium channel blocker, and a selective inhibitor of urokinase plasminogen activator (uPA). Amiloride selectively blocked the low threshold calcium channel in mouse neuroblastoma and chick dorsal root ganglion neurons[5]. ENaC inhibition by amiloride is used as an early intervention to halt the progression to full hypertension and cardiovascular disease in young adults with prehypertension. Following amiloride monotherapy for 4 weeks, a significant increase in serum aldosterone was observed (5.85±2.45 ng/dL)[6]. Amiloride inhibits Na+ uptake and competitively inhibits the catalytic activity of the urokinase-type plasminogen activator (u-PA) with a Ki value of 7μM[7]. Amiloride is able to reduce cell motility and thus lower proteinuria by inhibiting the expression of uPAR in podocytes[8].

Amiloride HCl dihydrate/盐酸阿米洛利二水合物 参考文献

[1]Tang CM, Presser F, Morad M. Amiloride selectively blocks the low threshold (T) calcium channel. Science. 1988;240(4849):213-5

[2]Bhagatwala J, Harris RA, Parikh SJ, et al. Epithelial sodium channel inhibition by amiloride on blood pressure and cardiovascular disease risk in young prehypertensives. J Clin Hypertens (Greenwich). 2014;16(1):47-53

[3]Vassalli JD, Belin D. Amiloride selectively inhibits the urokinase-type plasminogen activator. FEBS Lett. 1987;214(1):187-91

[4]Xu LB, Chi N, Shi W. Amiloride, a urokinase-type plasminogen activator receptor (uTPA) inhibitor, reduces proteinurea in podocytes. Genet Mol Res. 2015;14(3):9518-29

[5]Tang CM, Presser F, Morad M. Amiloride selectively blocks the low threshold (T) calcium channel. Science. 1988 Apr 8;240(4849):213-5. doi: 10.1126/science.2451291. PMID: 2451291.

[6]Bhagatwala J, Harris RA, Parikh SJ, Zhu H, Huang Y, Kotak I, Seigler N, Pierce GL, Egan BM, Dong Y. Epithelial sodium channel inhibition by amiloride on blood pressure and cardiovascular disease risk in young prehypertensives. J Clin Hypertens (Greenwich). 2014 Jan;16(1):47-53. doi: 10.1111/jch.12218. Epub 2013 Oct 31. PMID: 24410943; PMCID: PMC8031874.

[7]Vassalli JD, Belin D. Amiloride selectively inhibits the urokinase-type plasminogen activator. FEBS Lett. 1987 Apr 6;214(1):187-91. doi: 10.1016/0014-5793(87)80039-x. PMID: 3106085.

[8]Xu LB, Chi N, Shi W. Amiloride, a urokinase-type plasminogen activator receptor (uTPA) inhibitor, reduces proteinurea in podocytes. Genet Mol Res. 2015 Aug 14;14(3):9518-29. doi: 10.4238/2015.August.14.15. PMID: 26345885.

Amiloride HCl dihydrate/盐酸阿米洛利二水合物 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.31mL

0.66mL

0.33mL

16.55mL

3.31mL

1.66mL

33.10mL

6.62mL

3.31mL

Amiloride HCl dihydrate/盐酸阿米洛利二水合物 技术信息

CAS号17440-83-4
分子式C6H13Cl2N7O3
分子量 302.12
SMILES Code O=C(C1=NC(Cl)=C(N)N=C1N)NC(N)=N.[H]Cl.[H]O[H].[H]O[H]
MDL No. MFCD00211292
别名 MK-870 hydrochloride dihydrate; Amiloride hydrochloride dihydrate; Modamide.; Midoride; Midamor; Amiloride Hydrochloride; MK870
运输蓝冰
InChI Key LTKVFMLMEYCWMK-UHFFFAOYSA-N
Pubchem ID 68540
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

DMSO: 85 mg/mL(281.35 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 2 mg/mL(6.62 mM),配合低频超声助溶

动物实验配方

PO 0.5% CMC-Na 41 mg/mL suspension

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