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Purity: ≥98%
Rimeporide (also known as EMD-87580) is a novel, potent and selective inhibitor of the sodium/hydrogen Na+/H+ exchanger (NHE-1) with a potential to be used as a therapeutic agent for the treatment of heart failure and for patients with Duchenne muscular dystrophy.
| ln Vitro |
Rimeporide (EMD-87580) shows promise as a muscle protectant whose mode of action means it is independent of mutations. It has been demonstrated that blocking NHE-1 activity reduces intracellular Na+ and Ca2+ overload as well as pH. Rimeporide (EMD-87580) represents a new treatment option for Duchenne muscular dystrophy (DMD) [1].
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| References | |
| Additional Infomation |
Rimeporide has been used in trials studying the treatment of Muscular Dystrophy, Duchenne.
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| Molecular Formula |
C11H15N3O5S2
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|---|---|
| Molecular Weight |
333.3839
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| Exact Mass |
333.045
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| Elemental Analysis |
C, 39.63; H, 4.54; N, 12.60; O, 24.00; S, 19.23
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| CAS # |
187870-78-6
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| Related CAS # |
Rimeporide hydrochloride;187870-95-7
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| PubChem CID |
9799487
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| Appearance |
White to off-white solid powder
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| LogP |
2.961
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
21
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| Complexity |
638
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NC(N)=N)C1=CC(S(=O)(C)=O)=C(S(=O)(C)=O)C=C1C
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| InChi Key |
GROMEQPXDKRRIE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H15N3O5S2/c1-6-4-8(20(2,16)17)9(21(3,18)19)5-7(6)10(15)14-11(12)13/h4-5H,1-3H3,(H4,12,13,14,15)
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| Chemical Name |
N-(diaminomethylidene)-2-methyl-4,5-bis(methylsulfonyl)benzamide
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| Synonyms |
EMD87580; EMD-87580; EMD 87580;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~20 mg/mL (~59.99 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.24 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9996 mL | 14.9979 mL | 29.9958 mL | |
| 5 mM | 0.5999 mL | 2.9996 mL | 5.9992 mL | |
| 10 mM | 0.3000 mL | 1.4998 mL | 2.9996 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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