[CAS NO. 1222781-70-5] ML133 HCl
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PRODUCTS SPECIFICATIONS [1222781-70-5]
Catalog
SLK-S2825
Brand
Selleck
CAS
1222781-70-5
DESCRIPTION [1222781-70-5]
Overview
| MDL | MFCD20921521 |
|---|---|
| Molecular Weight | 313.82 |
| Molecular Formula | C19H19NO.HCl |
| SMILES | COC1=CC=C(C=C1)CNCC2=C3C=CC=CC3=CC=C2.[H]Cl |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1865 mL | 15.9327 mL | 31.8654 mL |
| 5 mM | 0.6373 mL | 3.1865 mL | 6.3731 mL |
| 10 mM | 0.3187 mL | 1.5933 mL | 3.1865 mL |
| 50 mM | 0.0637 mL | 0.3187 mL | 0.6373 mL |
Description
ML133 HCl is a selective potassium channel inhibitor for with of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on K1.1 and weak activity for K4.1 and K7.1.
Targets
| Kir2.1 [1] |
| 290 nM |
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 K2.1 in HEK 293 cells. M1 and/or M2 transmembrane domains contain the critical molecular determinant for ML133 inhibition of K2.1, especially D172 and I176.
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