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    ML133 HCl
    ML133 HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0210
    CAS #: 1222781-70-5Purity ≥98%

    Description: ML133 HCl, the hydrochloride salt of ML-133, is a novel, potent and selective inhibitor of the inward-rectifier potassium channel 2 (Kir2) identified from a high-throughput screening (HTS) of more than 300,000 small molecules. It inhibits Kir2.1 with an IC50 of 1.8 μM (at pH 7.4) and 290 nM (at pH 8.5), and shows no/little effect on Kir1.1, Kir4.1 and Kir7.1. The K(ir) inward rectifying potassium channels have a broad tissue distribution and are implicated in a variety of functional roles.  

    References: ACS Chem Biol. 2011 Aug 19;6(8):845-56. 

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    Molecular Weight (MW)313.82 
    FormulaC19H19NO.HCl 
    CAS No.1222781-70-5 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 63 mg/mL (200.8 mM)
    Water: <1 mg/mL
    Ethanol: 6 mg/mL (19.1 mM) 
    InChI Key NGQIBUUFXDPHKT-UHFFFAOYSA-N
    SynonymsML-133 HCl; ML133 HCl; ML 133 HCl; ML133 hydrochloride; ML 133 hydrochloride; ML-133 hydrochloride; 1-(4-methoxyphenyl)-N-(naphthalen-1-ylmethyl)methanamine hydrochloride, CID 781301 hydrochloride, N-(4-methoxybenzyl)-1-(naphthalen-1-yl)methanamine hydrochloride, SID 85281105 hydrochloride, VU0404943-1 hydrchloride


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    In Vitro

    In vitro activity: The ratio of total concentration of extracellular ML133 versus intracellular ML133 is 1:0.13 at pH 6.5, 1:9.09 at pH 8.5. ML133 is clean against 3A4 and 2C9 (IC50 >30 μM), displays moderate inhibition of 1A2 (IC50 = 3.3 μM) but proves to be a potent inhibitor of 2D6 (IC50 = 0.13 μM) in CYP450 assay. ML133 is highly protein bound (>99%) in both human and rat and also displays high intrinsic clearance in both species. ML133 (10 μM) is not displaced by K+ influx from the wild-type Kir2.1 in HEK 293 cells. M1 and/or M2 transmembrane domains contain the critical molecular determinant for ML133 inhibition of Kir2.1, especially D172 and I176.


    Kinase Assay: ML133 hydrochloride is a selective inhibitor of the Kir2 family of inward rectifier (IRK, KCNJ) potassium channels. ML133 inhibits Kir2.1 with IC50 of 1.8 μM at pH 7.4 and 290 nM at pH8.5. It exhibits little selectivity against other members of Kir2.x family channels, but has no effect on Kir1.1 (IC50 > 300 μM), and displays weak activity for Kir4.1 (76 μM) and Kir7.1 (33 μM), making ML133 the most selective small molecule inhibitor of the Kir family reported to date. It also showed modest selectivity versus hERG and a larger panel of GPCRs, ion channels and transporters.


    Cell Assay: ML133, which inhibits Kir2.1 with IC50 of 1.8 μM at pH 7.4 and 290 nM at pH 8.5, but exhibits little selectivity against other members of Kir2.x family channels. ML133 has no effect on Kir1.1 (IC50 > 300 μM), and displays weak activity for Kir4.1 (76 μM) and Kir7.1 (33 μM), making ML133 the most selective small molecule inhibitor of the Kir family reported to date.

    In VivoN/A
    Animal modelN/A
    Formulation & DosageN/A
    ReferencesACS Chem Biol. 2011 Aug 19;6(8):845-56.  


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    ML133 HCl


    Structural model of an inward rectifier potassium channel based on the Kir2.2 crystal structure, highlighting the tetrameric structure.   2011 Aug 19;6(8):845-56.

     ML133 HCl


    Structures and activities of representative Kir small molecule inhibitors.  2011 Aug 19;6(8):845-56.

     ML133 HCl


    Characterization of a novel Kir2.1 inhibitor, 2011 Aug 19;6(8):845-56.

     ML133 HCl


    Design and chemical lead optimization strategy for CID17367817, 11/ML133. A) diversity-oriented modular approach to survey three regions of 11;  2011 Aug 19;6(8):845-56.

     ML133 HCl


    Chimeric channels reveal critical domain(s) in Kir2.1 mediating ML133 inhibition.  2011 Aug 19;6(8):845-56.

     ML133 HCl


    Identification of the critical residuals for ML133 inhibition of Kir2.1.  2011 Aug 19;6(8):845-56.


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