Amiloride hydrochloride

Modify Date: 2024-01-02 18:29:15

Amiloride hydrochloride Structure
Amiloride hydrochloride structure
Common Name Amiloride hydrochloride
CAS Number 2016-88-8 Molecular Weight 266.088
Density 2.11 g/cm3 Boiling Point 628.1ºC at 760 mmHg
Molecular Formula C6H9Cl2N7O Melting Point 293-294°C
MSDS N/A Flash Point 333.7ºC

 Use of Amiloride hydrochloride


Amiloride (hydrochloride) is an epithelial sodium channel (ENaC) inhibitor and a competitive inhibitor of Urokinase-type plasminogen activator (uPA).

 Names

Name amiloride hydrochloride
Synonym More Synonyms

 Amiloride hydrochloride Biological Activity

Description Amiloride (hydrochloride) is an epithelial sodium channel (ENaC) inhibitor and a competitive inhibitor of Urokinase-type plasminogen activator (uPA).
Related Catalog
Target

ENaC, uPA[1]

In Vitro Amiloride blocks δβγ channels with an IC50 of 2.6 μM. The Ki of amiloride for δβγ ENaC is 26-fold that of αβγ channels (0.1 μM for αβγ ENaC). Amiloride blockade of δβγ ENaC is much more voltage dependent compared with the αβγ channel. The Ki of amiloride for δαβγ channels is 920 and 13.7 μM at −120 and +80 mV, respectively, which significantly differs from that of both αβγ and δβγ channels[1]. 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+]. Amiloride is an even weaker inhibitor of the Na+/Ca2+ exchanger (NCX), with an IC50 of 1 mM. Amiloride (1 μM) and submicromolar doses of Benzamil (30 nM), doses known to inhibit the ENaC, inhibit the myogenic vasoconstriction response to increasing perfusion pressure by blocking the activity of ENaC proteins. Amiloride completely inhibits Na+ influx in doses known to be relatively specific for ENaC (1.5 μM) in vascular smooth muscle cells (VSMC)[2].
In Vivo Amiloride (1 mg/kg/day) subcutaneously is found to reverse the initial increases in collagen deposition and prevent any further increases in the DOCA-salt hypertensive rat. Amiloride delays the onset of proteinuria and improved brain and kidney histologic scores in the saline-drinking, stroke-prone spontaneously hypertensive rats (SHRSP) compared with controls. Amiloride antagonizes or prevents actions of aldosterone in these cells and in cardiovascular and renal tissues in animals with salt-dependent forms of hypertension[2].
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.

 Chemical & Physical Properties

Density 2.11 g/cm3
Boiling Point 628.1ºC at 760 mmHg
Melting Point 293-294°C
Molecular Formula C6H9Cl2N7O
Molecular Weight 266.088
Flash Point 333.7ºC
Exact Mass 265.024567
PSA 156.79000
LogP 2.07300
Vapour Pressure 1.08E-15mmHg at 25°C
Storage condition Store at RT
Water Solubility H2O: 50 mg/mL, clear, yellow-green | <0.1 g/100 mL at 19.5 ºC

 MSDS

Material Safety Data Sheet

Section1. Identification of the substance
Product Name: Amiloride HCl dihydrate
Synonyms:

Section2. Hazards identification
Harmful by inhalation, in contact with skin, and if swallowed.
H301:Toxic if swallowed
P264:Wash thoroughly after handling
P270:Do not eat, drink or smoke when using this product
P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician
P321:Specific treatment (see on this label)
P405:Store locked up

Section3. Composition/information on ingredients.
Ingredient name:Amiloride HCl dihydrate
CAS number:2016-88-8

Section4. First aid measures
Skin contact:Immediately wash skin with copious amounts of water for at least 15 minutes while removing
contaminated clothing and shoes. If irritation persists, seek medical attention.
Eye contact:Immediately wash skin with copious amounts of water for at least 15 minutes. Assure adequate
flushing of the eyes by separating the eyelids with fingers. If irritation persists, seek medical
attention.
Inhalation:Remove to fresh air. In severe cases or if symptoms persist, seek medical attention.
Ingestion:Wash out mouth with copious amounts of water for at least 15 minutes. Seek medical attention.

Section5. Fire fighting measures
In the event of a fire involving this material, alone or in combination with other materials, use dry
powder or carbon dioxide extinguishers. Protective clothing and self-contained breathing apparatus
should be worn.

Section6. Accidental release measures
Personal precautions: Wear suitable personal protective equipment which performs satisfactorily and meets local/state/national
standards.
Respiratory precaution:Wear approved mask/respirator
Hand precaution:Wear suitable gloves/gauntlets
Skin protection:Wear suitable protective clothing
Eye protection:Wear suitable eye protection
Methods for cleaning up: Mix with sand or similar inert absorbent material, sweep up and keep in a tightly closed container
for disposal. See section 12.
Environmental precautions: Do not allow material to enter drains or water courses.

Section7. Handling and storage
Handling:This product should be handled only by, or under the close supervision of, those properly qualified
in the handling and use of potentially hazardous chemicals, who should take into account the fire,
health and chemical hazard data given on this sheet.
Storage:Store in closed vessels.

Section8. Exposure Controls / Personal protection
Engineering Controls: Use only in a chemical fume hood.
Personal protective equipment: Wear laboratory clothing, chemical-resistant gloves and safety goggles.
General hydiene measures: Wash thoroughly after handling. Wash contaminated clothing before reuse.

Section9. Physical and chemical properties
Appearance:Not specified
Boiling point:No data
Melting point:No data
Flash point:No data
Density:No data
Molecular formula:C6H8ClN7O.ClH.2H2O
Molecular weight:302.1

Section10. Stability and reactivity
Conditions to avoid: Heat, flames and sparks.
Materials to avoid: Oxidizing agents.
Possible hazardous combustion products: Carbon monoxide, nitrogen oxides, hydrogen chloride.

Section11. Toxicological information
No data.

Section12. Ecological information
No data.

Section13. Disposal consideration
Arrange disposal as special waste, by licensed disposal company, in consultation with local waste
disposal authority, in accordance with national and regional regulations.

Section14. Transportation information
UN Number:UN2811 Class: 6.1 Packing group: III
Proper shipping name: TOXIC SOLIDS, ORGANIC, N.O.S. (Amiloride HCl dihydrate)

Section15. Regulatory information
No chemicals in this material are subject to the reporting requirements of SARA Title III, Section
302, or have known CAS numbers that exceed the threshold reporting levels established by SARA
Title III, Section 313.


SECTION 16 - ADDITIONAL INFORMATION
N/A

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UQ2275500
CHEMICAL NAME :
Pyrazinecarboxamide, N-amidino-3,5-diamino-6-chloro-, monohydrochloride
CAS REGISTRY NUMBER :
2016-88-8
LAST UPDATED :
199504
DATA ITEMS CITED :
2
MOLECULAR FORMULA :
C6-H8-Cl-N7-O.Cl-H
MOLECULAR WEIGHT :
266.12

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

TYPE OF TEST :
Mutation in microorganisms
TEST SYSTEM :
Bacteria - Salmonella typhimurium
DOSE/DURATION :
1 mg/plate
REFERENCE :
EMMUEG Environmental and Molecular Mutagenesis. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.10- 1987- Volume(issue)/page/year: 19(Suppl 21),2,1992 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3814 No. of Facilities: 32 (estimated) No. of Industries: 2 No. of Occupations: 9 No. of Employees: 4480 (estimated) No. of Female Employees: 1822 (estimated)

 Safety Information

Hazard Codes T:Toxic
Risk Phrases R25
Safety Phrases S36-S45
RIDADR UN 2811 6.1/PG 3
WGK Germany 3
RTECS UQ2275500
Packaging Group II
Hazard Class 6.1(a)
HS Code 29339980

 Customs

HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

GUANAMPRAZINE
amiprazidine
2-Pyrazinecarboxamide, 3,5-diamino-N-(aminoiminomethyl)-6-chloro-, hydrochloride (1:1)
3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide hydrochloride
N-Amidino-3,5-diamino-6-chloropyrazinecarboxamide hydrochloride hydrate
3,5-Diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide Hydrochloride Hydrate
Amiloridhydrochlorid
N-amidino-3,5-diamino-6-chloro-pyrazinecarboxamide hydrochloride
AMIPRAMIDIN
Amiloride HCl
3,5-Diamino-N-carbamimidoyl-6-chloro-2-pyrazinecarboxamide hydrochloride (1:1)
3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide chlorhydrate
N-amidino-3,5-diamino-6-chloropyrazinecarboxamide hydrochloride
3,5-diamino-N-[amino(imino)methyl]-6-chloropyrazine-2-carboxamide hydrochloride
Arumil
AMipraMidine
HCL AMILORIDE HCL
UNII-7M458Q65S3
Midamor
Pyrazinecarboxamide, 3,5-diamino-N-(aminoiminomethyl)-6-chloro-, monohydrochloride
3,5-Diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide hydrochloride (1:1)
AMIPRAMIZIDE
amiloride monohydrochloride
amiloridechloride
Amiloride (hydrochloride)
Guanamprazine hydrochloride
AMipraMizi
EINECS 217-958-2
MFCD03703482
2-pyrazinecarboxamide, 3,5-diamino-N-(aminoiminomethyl)-6-chloro-, monohydrochloride
Amiloride hydrochloride
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