ML133 HClPotassium channel inhibitor for Kir2.1 CAS# 1222781-70-5 |
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Quality Control & MSDS
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| Cas No. | 1222781-70-5 | SDF | Download SDF |
| PubChem ID | 44247466 | Appearance | Powder |
| Formula | C19H20ClNO | M.Wt | 313.82 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 125 mg/mL (398.32 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 1-(4-methoxyphenyl)-N-(naphthalen-1-ylmethyl)methanamine;hydrochloride | ||
| SMILES | COC1=CC=C(C=C1)CNCC2=CC=CC3=CC=CC=C32.Cl | ||
| Standard InChIKey | NGQIBUUFXDPHKT-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C19H19NO.ClH/c1-21-18-11-9-15(10-12-18)13-20-14-17-7-4-6-16-5-2-3-8-19(16)17;/h2-12,20H,13-14H2,1H3;1H | ||
| 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. |
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| 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. |
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| 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. | ||
| Description | Selective blocker of inwardly rectifying Kir2 potassium channels (IC50 values are 1.8, 2.8, 2.9 and 4.0 μM at pH 7.4 for mKir2.1, hKir2.6, hKir2.2 and hKir2.3 respectively). Exhibits no effect on rKir1.1 (IC50 > 300 μM); displays weak activity at hKir7.1 and rKir4.1 (IC50 values are 33 and 76 μM). |
ML133 HCl Dilution Calculator
ML133 HCl Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.1865 mL | 15.9327 mL | 31.8654 mL | 63.7308 mL | 79.6635 mL |
| 5 mM | 0.6373 mL | 3.1865 mL | 6.3731 mL | 12.7462 mL | 15.9327 mL |
| 10 mM | 0.3187 mL | 1.5933 mL | 3.1865 mL | 6.3731 mL | 7.9664 mL |
| 50 mM | 0.0637 mL | 0.3187 mL | 0.6373 mL | 1.2746 mL | 1.5933 mL |
| 100 mM | 0.0319 mL | 0.1593 mL | 0.3187 mL | 0.6373 mL | 0.7966 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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ML133 is a selective potassium channel inhibitor for Kir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on Kir1.1 and weak activity for Kir4.1 and Kir7.1.
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Selective inhibition of the K(ir)2 family of inward rectifier potassium channels by a small molecule probe: the discovery, SAR, and pharmacological characterization of ML133.[Pubmed:21615117]
ACS Chem Biol. 2011 Aug 19;6(8):845-56.
The K(ir) inward rectifying potassium channels have a broad tissue distribution and are implicated in a variety of functional roles. At least seven classes (K(ir)1-K(ir)7) of structurally related inward rectifier potassium channels are known, and there are no selective small molecule tools to study their function. In an effort to develop selective K(ir)2.1 inhibitors, we performed a high-throughput screen (HTS) of more than 300,000 small molecules within the MLPCN for modulators of K(ir)2.1 function. Here we report one potent K(ir)2.1 inhibitor, ML133, which inhibits K(ir)2.1 with an IC(50) of 1.8 muM at pH 7.4 and 290 nM at pH 8.5 but exhibits little selectivity against other members of Kir2.x family channels. However, ML133 has no effect on K(ir)1.1 (IC(50) > 300 muM) and displays weak activity for K(ir)4.1 (76 muM) and K(ir)7.1 (33 muM), making ML133 the most selective small molecule inhibitor of the K(ir) family reported to date. Because of the high homology within the K(ir)2 family-the channels share a common design of a pore region flanked by two transmembrane domains-identification of site(s) critical for isoform specificity would be an important basis for future development of more specific and potent K(ir) inhibitors. Using chimeric channels between K(ir)2.1 and K(ir)1.1 and site-directed mutagenesis, we have identified D172 and I176 within M2 segment of K(ir)2.1 as molecular determinants critical for the potency of ML133 mediated inhibition. Double mutation of the corresponding residues of K(ir)1.1 to those of K(ir)2.1 (N171D and C175I) transplants ML133 inhibition to K(ir)1.1. Together, the combination of a potent, K(ir)2 family selective inhibitor and identification of molecular determinants for the specificity provides both a tool and a model system to enable further mechanistic studies of modulation of K(ir)2 inward rectifier potassium channels.
