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Membrane transporter/Ion channel Sodium Channel Rimeporide hydrochloride

Rimeporide hydrochloride

Catalog No. T5333   CAS 187870-95-7
Synonyms: EMD-87580 hydrochloride, EMD-87580 hydrochloride

Rimeporide (EMD-87580) is a potent and selective Sodium hydrogen exchange 1 (NHE-1) inhibitor.

Rimeporide hydrochloride, CAS 187870-95-7
Pack Size Availability Price/USD Quantity
1 mg In Stock 156.00
5 mg In Stock 365.00
10 mg In Stock 491.00
25 mg In Stock 824.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Rimeporide (EMD-87580) is a potent and selective Sodium hydrogen exchange 1 (NHE-1) inhibitor.
Targets&IC50 NHE-1,  
Cell Research
To induce hypertrophy, myocytes were treated for 10 min or 24 h as appropriate and noted under Results with 10 μM phenylephrine in the absence or presence of the following agents: the NHE-1 inhibitor EMD87580 (5 μM) or cariporide (5 μM), the JNK1/2 inhibitor SP600125, the p38 inhibitor SB203580, the ERK1/2 inhibitor PD98059 (all at 10 μM), and the reverse mode Na+-Ca2+ exchange inhibitor KB-R7943 or SN-6 (both at 10 μM). All drugs were added 30 min before the addition of phenylephrine [1].
Animal Research
Two groups were studied. The treatment group (n = 5) received EMD 87580 at a dose of 5 mg/kg IV bolus 5 min before aortic cross-clamping and 10 mol/L EMD 87580 in the cardioplegic solution. The control group (n = 9) received the same volume of saline vehicle. Systemic pretreatment was used to ensure drug availability during the ischemic period prior to CPA. Direct infusion via cardioplegia ensures drug delivery at the time of ischemia (CPA), and it decreases the variability of drug delivery that may occur during the hemodilution with CPB initiation. Incorporation into the cardioplegia also minimizes the potential variable of drug/extracorporeal circuit interactions. Using this dosing regimen, the plasma concentration of EMD 87580 was in the 2,500 to 3,000 ng/mL range at 10 min after CPB. This concentration has been shown to be effective at Na+/H+ exchanger inhibition in vitro [2].
Synonyms EMD-87580 hydrochloride , EMD-87580 hydrochloride
Purity 99.84%
Molecular Weight 369.84
Formula C11H16ClN3O5S2
CAS No. 187870-95-7

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 18.5 mg/mL (50 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Stanbouly S, et al. Sodium hydrogen exchange 1 (NHE-1) regulates connexin 43 expression in cardiomyocytes via reverse mode sodium calcium exchange and c-Jun NH2-terminal kinase-dependent pathways. J Pharmacol Exp Ther. 2008 Oct;327(1):105-13. 2. Cox CS Jr, et al. Improved myocardial function using a Na+/H+ exchanger inhibitor during cardioplegic arrest and cardiopulmonary bypass. Chest. 2003 Jan;123(1):187-94.

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