CAS 2609-46-3|Amiloride

Introduction：Basic information about CAS 2609-46-3|Amiloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Amiloride BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Customs
6. Synonyms

Common Name	Amiloride
CAS Number	2609-46-3	Molecular Weight	229.62700
Density	2.11g/cm3	Boiling Point	628.1ºC at 760 mmHg
Molecular Formula	C₆H₈ClN₇O	Melting Point	/
MSDS	/	Flash Point	333.7ºC

Names

Name	amiloride
Synonym	More Synonyms

Amiloride BiologicalActivity

Description	Amiloride is a relatively selective inhibitor of the epithelial sodium channel (ENaC), used in the management of hypertension and congestive heart failure.
Related Catalog	Signaling Pathways >>Membrane Transporter/Ion Channel >>Sodium ChannelResearch Areas >>Metabolic Disease
Target	Sodium channel
In Vitro	Amiloride blocks δβγ channels with an IC50 of 2.6 μM (58, 71, 75, 134, 148). 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	2.11g/cm3
Boiling Point	628.1ºC at 760 mmHg
Molecular Formula	C₆H₈ClN₇O
Molecular Weight	229.62700
Flash Point	333.7ºC
Exact Mass	229.04800
PSA	156.79000
LogP	1.27100
Vapour Pressure	1.08E-15mmHg at 25°C
Index of Refraction	1.884
InChIKey	XSDQTOBWRPYKKA-UHFFFAOYSA-N
SMILES	NC(N)=NC(=O)c1nc(Cl)c(N)nc1N

Safety Information

HS Code	2934999090

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

Amipramizide

Amiloridum

Amipramidin

Amyloride

EINECS 220-024-7

MFCD00077316

AMILORIDE

Midamor

3,5-diamino-6-chloro-N-(diaminomethylidene)pyrazine-2-carboxamide

Guanamprazin

3,5-diamino-6-chloro-pyrazine-2-carboxylic acid carbamimidoylamide

Amipramizid

Amilorida

Recommended......