| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg | |||
| Other Sizes |
| Targets |
KCNQ1-KCNE1 voltage-gated potassium channel complex (mediates the slowly activating delayed rectifier K+ current, IKs).
|
|---|---|
| ln Vitro |
In canine left ventricular myocytes, HMR 1556 suppresses Ito, ICa, L, and IKr with IC50 values of 33.9 μM, 27.5 μM, and 12.6 μM, respectively [1].
HMR-1556 inhibits IKs with IC50 values of 10.5 nM in canine left ventricular myocytes and 34 nM in guinea pig left ventricular myocytes. It shows little or no inhibition of Herg, Kv1.3 (KCNA3), Kv1.5 (KCNA5), Kir2.1 (KCNJ2), or HCN2 (BCNG2) currents in oocyte transfectants at relevant concentrations. In Xenopus oocytes expressing hKCNE1, IC50 is 120 nM. |
| ln Vivo |
In vivo, HMR-1556 has been used to study the role of IKs in cardiac electrophysiology and arrhythmias. As a selective IKs blocker, it prolongs cardiac action potential duration and has been investigated in models of long QT syndrome. Specific dosing regimens and detailed efficacy data are available in the literature.
|
| Enzyme Assay |
IKs channel activity is assessed using patch-clamp electrophysiology in cells or oocytes expressing KCNQ1 and KCNE1. Voltage-clamp protocols are used to activate IKs and measure current amplitude. IC50 values are calculated from dose-response curves. Selectivity is evaluated by testing against other potassium and calcium channels.
|
| Cell Assay |
Cellular activity is evaluated in cardiac myocytes or oocytes expressing KCNQ1-KCNE1. Cells are treated with HMR-1556 at various concentrations and IKs currents are measured by patch-clamp. Action potential duration is assessed in cardiac myocytes. Effects on other ion channels are evaluated to confirm selectivity.
|
| Animal Protocol |
In vivo efficacy is studied in animal models of cardiac arrhythmias. HMR-1556 is administered intravenously or orally. Electrocardiograms are recorded to measure QT interval prolongation. Arrhythmia susceptibility is assessed. The compound has been used to validate the role of IKs in cardiac repolarization and to model long QT syndrome.
|
| ADME/Pharmacokinetics |
HMR-1556 has a molecular formula of C17H24F3NO5S and molecular weight of 411.44. The compound is a chromanol derivative. It is soluble in DMSO. Detailed pharmacokinetic parameters including half-life, oral bioavailability, and plasma protein binding are available in the literature but not detailed in public search results.
|
| Toxicity/Toxicokinetics |
Safety data for HMR-1556 indicate it is a research compound for laboratory use only. As an IKs blocker, it may have cardiac effects including QT interval prolongation. The compound should be handled with appropriate safety precautions. Specific toxicological profiles are not extensively published.
|
| References | |
| Additional Infomation |
I(Ks) channel blocker; structure in the first source
HMR-1556 is a research tool compound for studying IKs channel function and cardiac electrophysiology. It is not approved for clinical use. The compound has been used to investigate the role of IKs in cardiac repolarization, long QT syndrome, and arrhythmias. Its high potency and selectivity make it a valuable pharmacological probe for potassium channel research. |
| Molecular Formula |
C17H24NO5F3S
|
|---|---|
| Molecular Weight |
411.43636
|
| Exact Mass |
425.148
|
| CAS # |
223749-46-0
|
| PubChem CID |
9887834
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.6
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
27
|
| Complexity |
605
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CC1(C(C(C2=C(O1)C=CC(=C2)OCCCC(F)(F)F)N(C)S(=O)(=O)C)O)C
|
| InChi Key |
SRZRLJWUQFIZRH-LSDHHAIUSA-N
|
| InChi Code |
InChI=1S/C17H24F3NO5S/c1-16(2)15(22)14(21(3)27(4,23)24)12-10-11(6-7-13(12)26-16)25-9-5-8-17(18,19)20/h6-7,10,14-15,22H,5,8-9H2,1-4H3/t14-,15+/m0/s1
|
| Chemical Name |
N-[(3R,4S)-3-hydroxy-2,2-dimethyl-6-(4,4,4-trifluorobutoxy)-3,4-dihydrochromen-4-yl]-N-methylmethanesulfonamide
|
| Synonyms |
HMR1556; HMR 1556; HMR-1556
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~243.05 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.08 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: 2.5 mg/mL (6.08 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (6.08 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 | 2.4305 mL | 12.1524 mL | 24.3049 mL | |
| 5 mM | 0.4861 mL | 2.4305 mL | 4.8610 mL | |
| 10 mM | 0.2430 mL | 1.2152 mL | 2.4305 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
