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ML133 hydrochloride (ML133 HCl) 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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $43 | In Stock | |
10 mg | $61 | In Stock | |
25 mg | $108 | In Stock | |
50 mg | $173 | In Stock | |
100 mg | $288 | In Stock | |
200 mg | $373 | In Stock | |
500 mg | $629 | In Stock | |
1 mL x 10 mM (in DMSO) | $48 | In Stock |
Description | ML133 hydrochloride (ML133 HCl) 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. |
Targets&IC50 | KIR2.1 (pH 8.5):290 nM, KIR2.1 (pH 7.4):1.8 μM |
In vitro | 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. [1] |
Alias | ML133 HCl |
Molecular Weight | 313.82 |
Formula | C19H19NO·HCl |
Cas No. | 1222781-70-5 |
Smiles | Cl.COC1=CC=C(CNCC2=CC=CC3=CC=CC=C23)C=C1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 16.67 mg/mL (53.11 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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