5-(N,N-HEXAMETHYLENE)-AMILORIDE
Synonym(s):HMA
- CAS NO.:1428-95-1
- Empirical Formula: C12H18ClN7O
- Molecular Weight: 311.77
- MDL number: MFCD00069211
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:32
What is 5-(N,N-HEXAMETHYLENE)-AMILORIDE?
Description
5-(N,N-hexamethylene)-Amiloride (HMA) is a derivative of amiloride with diverse biological activities. It is an allosteric antagonist of adenosine A2A receptors (Ki = 3.3 μM). HMA inhibits the cation-selective ion channel formed by the HIV-1 viral protein Vpu when used at a concentration of 50 μM, as well as budding of virus-like particles in HeLa cells expressing the HIV-1 proteins Gag and Vpu when used at a concentration of 10 μM. It also blocks the cation-selective ion channels formed by the hepatitis C virus (HCV) protein p7. HMA (40 μM) induces necrosis in and reduces the viability of MCF-7, MDA-MB-231, T47D, SK-BR-3, Met-1, and NDL breast cancer cells but not cardiomyocytes or uterine, pulmonary, and renal epithelial cells. HMA protects against post-ischemic contractile dysfunction and reduces coronary effluent creatine phosphokinase activity in a model of ischemia-reperfusion injury using isolated rat right ventricular free walls.
What are the applications of Application
5-(N,N-Hexamethylene)amiloride is an inhibitor of Na+/H+ antiport
Definition
ChEBI: A member of the class of pyrazines that is amiloride in which the two amino hydrogens at position N-5 are replaced by a hexamethylene moiety, resulting in the formation of an azepane ring.
Biochem/physiol Actions
Inhibitor of Na+/H+ antiport.
Properties of 5-(N,N-HEXAMETHYLENE)-AMILORIDE
Melting point: | 224-225 °C |
Density | 1.63±0.1 g/cm3(Predicted) |
storage temp. | 2-8°C |
solubility | DMF: 3mg/mL; DMSO: 10mg/mL; DMSO:PBS (pH 7.2) (1:4): 0.2mg/mL |
form | A crystalline solid |
pka | 8.81±0.46(Predicted) |
color | Light yellow to yellow |
Safety information for 5-(N,N-HEXAMETHYLENE)-AMILORIDE
Signal word | Danger |
Pictogram(s) |
Skull and Crossbones Acute Toxicity GHS06 |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P264:Wash hands thoroughly after handling. P264:Wash skin thouroughly after handling. P280:Wear protective gloves/protective clothing/eye protection/face protection. P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician. |
Computed Descriptors for 5-(N,N-HEXAMETHYLENE)-AMILORIDE
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