Ethacrynic Acid
Ethacrynic acid is one of the most used loop diuretics, acting by inhibiting NKCC2 which is specifically found in the thick ascending loop of Henle in the kidneys. Inhibition of NKCC2 significantly increases the concentrations of Na+, K+, and Cl− in the tubule, and reduces hypertonicity in the surrounding interstitium, causing less water to be reabsorbed into the blood. Eventually, more urine will be produced and excreted, and a decrease in blood volume can be achieved. Loop diuretics have been used for the treatment of fluid overload/edema in congestive heart failure, acute pulmonary edema, nephrotic syndrome, hepatic ascites, renal failure, as well as other edematous disorders.
References:
1. Vardanyan R, Hruby V. Synthesis of Best-Seller Drugs. Chapter 21 - Diuretics, 2016, 317-327.
2. Zins GR, Walk RA, Gussin RZ, et al. The diuretic activity of ethacrynic acid in rats. Journal of Pharmacology and Experimental Therapeutics, 1968, 163(1): 210-215.
| Storage | Store at -20°C |
| M.Wt | 303.14 |
| Cas No. | 58-54-8 |
| Formula | C13H12Cl2O4 |
| Synonyms | MK 595,NSC 85791,NSC 624008 |
| Solubility | insoluble in H2O; ≥30.37 mg/mL in DMSO; ≥44.4 mg/mL in EtOH |
| Chemical Name | 2-(2,3-dichloro-4-(2-methylenebutanoyl)phenoxy)acetic acid |
| SDF | Download SDF |
| Canonical SMILES | O=C(O)COC1=CC=C(C(C(CC)=C)=O)C(Cl)=C1Cl |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Animal experiment:[2] | |
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Animal models |
Rats |
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Dosage form |
37.5 and 125 mg/kg Intravenous administration |
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Applications |
Single doses of 37.5 and 125 mg/kg increased water and potassium excretion 2-fold, sodium excretion 3-fold and chloride excretion 4-fold in relation to parallel control animals. Single dose activity was confined to the 1st hr after injection whereas effects persisted for the duration of observation when animals were primed with 25 mg/kg and sustained with 50 mg/kg/hr. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Vardanyan R, Hruby V. Synthesis of Best-Seller Drugs. Chapter 21 - Diuretics, 2016, 317-327. 2. Zins GR, Walk RA, Gussin RZ, et al. The diuretic activity of ethacrynic acid in rats. Journal of Pharmacology and Experimental Therapeutics, 1968, 163(1): 210-215. |
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