Size | Price | |
---|---|---|
50mg | ||
100mg | ||
250mg |
ln Vitro |
Amiloride has an IC50 of 2.6 μM for blocking δβγ channels (58, 71, 75, 134, 148). Amiloride's Ki for δβγ ENaC channels is 26 times greater than that of αβγ channels (0.1 μM for αβγ ENaC). Compared to αβγ channels, amiloride's blockade of δβγ ENaC is more voltage-dependent. In contrast to the Ki values of αβη and δβγ channels, the amiloride Ki values for δαβγ channels are 920 and 13.7 μM at -120 and +80 mV, respectively [1]. Amiloride is an inhibitor of the epithelial sodium channel (ENaC) that is relatively selective. Its IC50, or the dose needed to cause 50% blockage of the ion channel, falls between 0.1 and 0.5 μM. With an IC50 as low as 3 μM in the presence of low external [Na+] and as high as 1 mM in the case of high [Na+], amiloride is a relatively weak inhibitor of the Na+/H+ exchanger (NHE). Amiloride has an IC50 of 1 mM, making it a weaker inhibitor of the Na+/Ca2+ exchanger (NCX). It is known that amiloride (1 μM) and submicromolar dosages of benzamil (30 nM) inhibit ENaC. This means that by preventing the ENaC protein from acting, they prevent the myogenic vasoconstrictive response to elevated perfusion pressure. In vascular smooth muscle cells (VSMC), amiloride totally blocks Na+ inflow at a dosage that is known to be relatively selective for ENaC (1.5 μM) [2].
|
---|---|
ln Vivo |
In saline-drinking, stroke-prone spontaneously hypertensive rats (SHRSP) compared to controls, amiloride improved brain and kidney histological scores and reversed the initial increase in collagen deposition and prevented further increases in this tissue via subcutaneous injection (1 mg/kg/day) [2]. Amiloride also antagonizes or blocks the effects of aldosterone in these cells as well as in cardiovascular and renal tissue in animals with salt-dependent hypertension.
|
References |
[1]. Ji, H.L., et al. delta ENaC: a novel divergent amiloride-inhibitable sodium channel. Am J Physiol Lung Cell Mol Physiol, 2012. 303(12): p. L1013-26.
[2]. 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. [3]. Giamarchi A, 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. |
Molecular Formula |
C6H8CLN7O
|
---|---|
Molecular Weight |
229.63
|
Exact Mass |
229.0479
|
CAS # |
2609-46-3
|
Related CAS # |
Amiloride hydrochloride;2016-88-8;Amiloride hydrochloride dihydrate;17440-83-4
|
SMILES |
O=C(C1=NC(Cl)=C(N)N=C1N)NC(N)=N
|
Synonyms |
MK-870 MK 870 MK870
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
---|
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.3548 mL | 21.7742 mL | 43.5483 mL | |
5 mM | 0.8710 mL | 4.3548 mL | 8.7097 mL | |
10 mM | 0.4355 mL | 2.1774 mL | 4.3548 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.