Compound Selection

Formula: C6H8ClN7O

MW: 229.63

Salt: HCl; H2O

CAS: 2016-88-8

MDL NUMBER: MFCD00077316

IUPAC: (3,5-diamino-6-chloropyrazin-2-yl)-N-(???methyl)carboxamide

Smiles: c1(nc(c(N)nc1N)Cl)C(NC(=N)N)=O

THERAPEUTIC CATEGORY: Diuretic

ACCEPTORS: 1

DONORS: 8

ROTATION BONDS: 1

N+O: 8

Chiral Centers: 0

LogP: -2.9

LogS: -1.53

LIPINSKI: 3

Synonyms: amiloridechloride;amiprazidine;n-amidino-3,5-diamino-6-chloro-pyrazinecarboxamidmonohydrochloride;N-AMIDINO-3,5-DIAMINO-6-CHLOROPYRAZINECARBOXAMIDE HYDROCHLORIDE;GUANAMPRAZINE;AMIPRAMIDIN;AMIPRAMIZIDE;AMILORIDE HCL

CAS:2016-88-8

MF:C6H8ClN7O.ClH

MW:266.09

EINECS:217-958-2

Product Categories:Active Pharmaceutical Ingredients;Ion transporter and other ion channel;Ion Channels Amiloride hydrochloride

Chemical Properties: mp 293-294C storage temp. Store at RT solubility H2O: 50 mg/mL, clear, yellow-green form powder color yellow Water Solubility <0.1 g/100 mL at 19.5 C

CAS DataBase Reference: 2016-88-8(

CAS DataBase Reference: ) EPA Substance Registry SystemPyrazinecarboxamide, 3,5-diamino-N-(aminoiminomethyl)- 6-chloro-, monohydrochloride(2016-88-8) T,Xi Risk Statements 25-36/37/38 Safety Statements 36-45-26 RIDADR UN 2811 6.1/PG 3 WGK Germany 3 RTECS UQ2275500 HazardClass 6.1(a) PackingGroup II Amiloride hydrochloride Amiloride hydrochloride

Usage And Synthesis: UsageSodium channel blocker. Diuretic. General DescriptionCrystalline solid or very light yellow powder. Air & Water ReactionsInsoluble in water. Reactivity ProfileA halogenated amine and amide, acidic salt. In aqueous solution, behaves as a weak acid. Amines are chemical bases. They neutralize acids to form salts plus water. These acid-base reactions are exothermic. The amount of heat that is evolved per mole of amine in a neutralization is largely independent of the strength of the amine as a base. Amines may be incompatible with isocyanates, halogenated organics, peroxides, phenols (acidic), epoxides, anhydrides, and acid halides. Flammable gaseous hydrogen is generated by amines in combination with strong reducing agents, such as hydrides. Organic amides/imides react with azo and diazo compounds to generate toxic gases. Flammable gases are formed by the reaction of organic amides/imides with strong reducing agents. Amides are very weak bases (weaker than water). Imides are less basic yet and in fact react with strong bases to form salts. That is, they can react as acids. Mixing amides with dehydrating agents such as P2O5 or SOCl2 generates the corresponding nitrile. The combustion of these compounds generates mixed oxides of nitrogen (NOx). Health HazardSYMPTOMS: Symptoms of exposure to Amiloride hydrochloride include headache, weakness, fatigue, back, chest, neck, shoulder or extremity pain; nausea, anorexia, vomiting, abdominal pain, hyperkalemia, paresthesias, shock, dizziness, coughing, shortness of breath, depression, nervousness, flaccid paralysis of the extremities, bradycardia, flatulence, skin rash, gas pain, constipation and dyspnea. Fire HazardFlash point data for Amiloride hydrochloride are not available; however, Amiloride hydrochloride is probably combustible. Biological ActivityNa + channel blocker. Defines the I 2A -amiloride sensitive and I 2B -amiloride insensitive imidazoline binding sites. Also inhibits TRPP3 channels. Amiloride hydrochloride

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