Amiloride HCl dihydrate

产品说明书

Print
Chemical Structure| 17440-83-4 同义名 : MK-870 hydrochloride dihydrate; Amiloride hydrochloride dihydrate; Modamide.; Midoride; Midamor; Amiloride Hydrochloride; MK870
CAS号 : 17440-83-4
货号 : A105627
分子式 : C6H13Cl2N7O3
纯度 : 97%
分子量 : 302.12
MDL号 : MFCD00211292
存储条件：

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

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

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

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].
实验方案
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
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.