Amiloride (MK-870)
(Synonyms: 阿米洛利; MK-870) 目录号 : GC31431
Amiloride (MK-870)是一种选择性T型钙通道阻滞剂、上皮钠通道(ENaC)和尿激酶型纤溶酶原激活物受体(uTPA)抑制剂,Ki =7 µM。
Cas No.:2609-46-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
|
Cell lines |
Podocytes |
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Preparation Method |
Mature podocytes were treated with 50 mg/L lipopolysaccharide and 50 mg/L amiloride. |
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Reaction Conditions |
50 mg/L amiloride;24h |
|
Applications |
Amiloride(MK-870) decreased uPAR expression (due to the presence of lipopolysaccharide) in podocytes. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6 male mice |
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Preparation Method |
Mice was intragastrically administered 10 mg/kg/d of amiloride 2 days ahead of the lipopolysaccharide injection. |
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Dosage form |
10 mg/kg/d amiloride;3days;i. g. |
|
Applications |
Amiloride might inhibit uPAR expression in podocytes of transient proteinuria induced by lipopolysaccharid in the mouse model. |
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References: [1]. Xu LB, Chi N, et,al.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. |
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Amiloride (MK-870) is a selective T-type calcium channel blocker and an inhibitor of epithelial sodium channels (ENaC) and urokinase-type plasminogen activator receptor (uTPA), Ki=7 µM. It is also polycystin-2 (PC2;TRPP2) channel blocker[1-3].
Amiloride(50 mg/L;24h) decreased uPAR expression (due to the presence of lipopolysaccharide) in podocytes[4].
Amiloride is a relatively selective inhibitor of the epithelial sodium channel (ENaC) with an IC50 (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 IC50 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+][1]. Amiloride(0.1-1mM) together with Bumetanide completely blocked cell transition through G1 and entry into S-phase in BALB/c 3T3 cells [5].
Amiloride(10 mg/kg/d;3days;i.g.) might inhibit uPAR expression in podocytes of transient proteinuria induced by lipopolysaccharid in the mouse model[4]. In ApoE(-/-) mice, administration of amiloride(high-fat diets with 0.5% (w/w) amiloride;4 weeks) significantly suppressed LPS-accelerated atherosclerosis and LPS-induced increase of NHE1 activity, and reversed LPS-induced down-regulation of Bcl-2 expression[6]. Amiloride(2mg/kg/d;30days;i.p.) treatment in tumor-bearing mice(The CT26 and LLC cachexia cell models)distinctly alleviated muscle atrophy and relieved cachexia-related features without affecting tumor growth[7].
References:
[1]. Teiwes J, Toto RD. Epithelial sodium channel inhibition in cardiovascular disease. A potential role for amiloride. Am J Hypertens. 2007 Jan;20(1):109-17. doi: 10.1016/j.amjhyper.2006.05.022. PMID: 17198922.
[2]. Tang CM, Presser F, et,al. Amiloride selectively blocks the low threshold (T) calcium channel. Science. 1988 Apr 8;240(4849):213-5. doi: 10.1126/science.2451291. PMID: 2451291.
[3]. Giamarchi A, Feng S, et,al. A polycystin-2 (TRPP2) dimerization domain essential for the function of heteromeric polycystin complexes. EMBO J. 2010 Apr 7;29(7):1176-91. doi: 10.1038/emboj.2010.18. Epub 2010 Feb 18. PMID: 20168298; PMCID: PMC2857461.
[4]. Xu LB, Chi N, et,al.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.
[5]. Panet R, Snyder D, et,al. Amiloride added together with bumetanide completely blocks mouse 3T3-cell exit from G0/G1-phase and entry into S-phase. Biochem J. 1986 Nov 1;239(3):745-50. doi: 10.1042/bj2390745. PMID: 3548704; PMCID: PMC1147349.
[6]. Cui GM, Zhao YX, et,al.Amiloride attenuates lipopolysaccharide-accelerated atherosclerosis via inhibition of NHE1-dependent endothelial cell apoptosis. Acta Pharmacol Sin. 2013 Feb;34(2):231-8. doi: 10.1038/aps.2012.155. Epub 2012 Dec 31. PMID: 23274414; PMCID: PMC4011619.
[7]. Zhou L, Zhang T, et,al.Amiloride ameliorates muscle wasting in cancer cachexia through inhibiting tumor-derived exosome release. Skelet Muscle. 2021 Jul 6;11(1):17. doi: 10.1186/s13395-021-00274-5. PMID: 34229732; PMCID: PMC8258996.
Amiloride (MK-870)是一种选择性T型钙通道阻滞剂、上皮钠通道(ENaC)和尿激酶型纤溶酶原激活物受体(uTPA)抑制剂,Ki =7 µM。它也是polycystin-2 (PC2;TRPP2)通道阻滞剂[1-3]。
Amiloride (50mg /L;24h)降低足细胞中由于脂多糖的存在而上调的uPAR的表达[4]。Amiloride是一种相对选择性的上皮钠通道(ENaC)抑制剂,其IC50在0.1 ~ 0.5 µM的浓度范围内。Amiloride是一种相对较差的Na+/H+交换剂(NHE)抑制剂,在低外部[Na+]存在时IC50低至3 µM,而在高外部[Na+]存在时IC50高达1 mM[1]。Amiloride (0.1-1mM)联合Bumetanide完全阻断BALB/c 3T3细胞从G0/ G1期退出进入S期的过程[5]。
Amiloride (10 mg/kg/d;3days;i.g.)可能抑制脂多糖诱导的小鼠短暂性蛋白尿足细胞中uPAR的表达[4]。在ApoE(-/-)小鼠中,给予Amiloride (含0.5% (w/w)阿米洛利的高脂饮食;4weeks)可显著抑制LPS加速的动脉粥样硬化和NHE1活性升高,逆转LPS诱导的Bcl-2表达下调[6]。Amiloride(2mg/kg/d;30days;i.p.)治疗荷瘤小鼠(CT26和LLC细胞小鼠模型)明显缓解肌肉萎缩和恶病质相关特征,但不影响肿瘤生长[7]。
| Cas No. | 2609-46-3 | SDF | |
| 别名 | 阿米洛利; MK-870 | ||
| Canonical SMILES | O=C(C1=NC(Cl)=C(N)N=C1N)NC(N)=N | ||
| 分子式 | C6H8ClN7O | 分子量 | 229.63 |
| 溶解度 | DMSO : 100 mg/mL (435.48 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.3548 mL | 21.7742 mL | 43.5483 mL |
| 5 mM | 0.871 mL | 4.3548 mL | 8.7097 mL |
| 10 mM | 0.4355 mL | 2.1774 mL | 4.3548 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。