ML 277

Selective Kv7.1 (KCNQ1) potassium channel activator; augments IKs current CAS# 1401242-74-7

ML 277

Catalog No. BCC7976----Order now to get a substantial discount!

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ML 277: 5mg $115 In Stock
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Chemical structure

ML 277

3D structure

Chemical Properties of ML 277

Cas No. 1401242-74-7 SDF Download SDF
PubChem ID 53347902 Appearance Powder
Formula C23H25N3O4S2 M.Wt 471.59
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 56 mg/mL (118.75 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name (2R)-N-[4-(4-methoxyphenyl)-1,3-thiazol-2-yl]-1-(4-methylphenyl)sulfonylpiperidine-2-carboxamide
SMILES CC1=CC=C(C=C1)S(=O)(=O)N2CCCCC2C(=O)NC3=NC(=CS3)C4=CC=C(C=C4)OC
Standard InChIKey OXQNLLVUVDAEHC-OAQYLSRUSA-N
Standard InChI InChI=1S/C23H25N3O4S2/c1-16-6-12-19(13-7-16)32(28,29)26-14-4-3-5-21(26)22(27)25-23-24-20(15-31-23)17-8-10-18(30-2)11-9-17/h6-13,15,21H,3-5,14H2,1-2H3,(H,24,25,27)/t21-/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of ML 277

DescriptionSelective Kv7.1 (KCNQ1) potassium channel activator (EC50 = 260 nM). Exhibits >100-fold selectivity versus KCNQ2, KCNQ4 and hERG potassium channels. Augments IKs current of cultured human cardiomyocytes and shortens action potential duration.

ML 277 Dilution Calculator

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ML 277 Molarity Calculator

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Preparing Stock Solutions of ML 277

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.1205 mL 10.6024 mL 21.2049 mL 42.4097 mL 53.0122 mL
5 mM 0.4241 mL 2.1205 mL 4.241 mL 8.4819 mL 10.6024 mL
10 mM 0.212 mL 1.0602 mL 2.1205 mL 4.241 mL 5.3012 mL
50 mM 0.0424 mL 0.212 mL 0.4241 mL 0.8482 mL 1.0602 mL
100 mM 0.0212 mL 0.106 mL 0.212 mL 0.4241 mL 0.5301 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on ML 277

Lumbar interbody fusion with utilization of recombinant human bone morphogenetic protein: a retrospective real-life study about 277 patients.[Pubmed:28281191]

Neurosurg Rev. 2018 Jan;41(1):189-196.

The purpose of this study was to report an independent real-life experience about the use of recombinant human bone morphogenetic protein 2 in lumbar interbody fusion with a special focus on complications. This is a retrospective single-center cohort study between 2007 and 2013 including 277 patients treated for anterior or posterior lumbar fusion with recombinant human bone morphogenetic protein 2. We report the complications occurring during the 12 first postoperative months and analyze the fusion rate on X-rays. There are 58 cases (22.8%) of clinical complications. In 15 cases (5.9%), these complications were related to the use of recombinant human bone morphogenetic protein 2. Only one patient (0.4%) required a new intervention due to recombinant human bone morphogenetic protein 2. Fusion rate at 1 year was 98%. The low rate of specific complication suggests that recombinant human bone morphogenetic protein 2 can be safe and effective in anterior and posterior interbody fusion when used with simple precautions.

Dynamic subunit stoichiometry confers a progressive continuum of pharmacological sensitivity by KCNQ potassium channels.[Pubmed:23650380]

Proc Natl Acad Sci U S A. 2013 May 21;110(21):8732-7.

Voltage-gated KCNQ1 (Kv7.1) potassium channels are expressed abundantly in heart but they are also found in multiple other tissues. Differential coassembly with single transmembrane KCNE beta subunits in different cell types gives rise to a variety of biophysical properties, hence endowing distinct physiological roles for KCNQ1-KCNEx complexes. Mutations in either KCNQ1 or KCNE1 genes result in diseases in brain, heart, and the respiratory system. In addition to complexities arising from existence of five KCNE subunits, KCNE1 to KCNE5, recent studies in heterologous systems suggest unorthodox stoichiometric dynamics in subunit assembly is dependent on KCNE expression levels. The resultant KCNQ1-KCNE channel complexes may have a range of zero to two or even up to four KCNE subunits coassembling per KCNQ1 tetramer. These findings underscore the need to assess the selectivity of small-molecule KCNQ1 modulators on these different assemblies. Here we report a unique small-molecule gating modulator, ML277, that potentiates both homomultimeric KCNQ1 channels and unsaturated heteromultimeric (KCNQ1)4(KCNE1)n (n < 4) channels. Progressive increase of KCNE1 or KCNE3 expression reduces efficacy of ML277 and eventually abolishes ML277-mediated augmentation. In cardiomyocytes, the slowly activating delayed rectifier potassium current, or IKs, is believed to be a heteromultimeric combination of KCNQ1 and KCNE1, but it is not entirely clear whether IKs is mediated by KCNE-saturated KCNQ1 channels or by channels with intermediate stoichiometries. We found ML277 effectively augments IKs current of cultured human cardiomyocytes and shortens action potential duration. These data indicate that unsaturated heteromultimeric (KCNQ1)4(KCNE1)n channels are present as components of IKs and are pharmacologically distinct from KCNE-saturated KCNQ1-KCNE1 channels.

Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator.[Pubmed:22910039]

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5936-41.

A high-throughput screen utilizing a depolarization-triggered thallium influx through KCNQ1 channels was developed and used to screen the MLSMR collection of over 300,000 compounds. An iterative medicinal chemistry approach was initiated and from this effort, ML277 was identified as a potent activator of KCNQ1 channels (EC(50)=260 nM). ML277 was shown to be highly selective against other KCNQ channels (>100-fold selectivity versus KCNQ2 and KCNQ4) as well as against the distantly related hERG potassium channel.

Description

ML277(CID53347902) is a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator with EC50 of 270 nM.

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