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ML133 hydrochloride

Catalog No. T6592   CAS 1222781-70-5
Synonyms: ML133 HCl

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.

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ML133 hydrochloride Chemical Structure
ML133 hydrochloride, CAS 1222781-70-5
Pack Size Availability Price/USD Quantity
5 mg In stock $ 43.00
10 mg In stock $ 61.00
25 mg In stock $ 108.00
50 mg In stock $ 173.00
100 mg In stock $ 288.00
200 mg In stock $ 373.00
500 mg In stock $ 629.00
1 mL * 10 mM (in DMSO) In stock $ 48.00
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Purity: 99.81%
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Biological Description
Chemical Properties
Storage & Solubility Information
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]
Synonyms ML133 HCl
Molecular Weight 313.82
Formula C19H19NO·HCl
CAS No. 1222781-70-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 31.4 mg/mL (100 mM)

TargetMolReferences and Literature

1. Wang HR, et al. ACS Chem Biol, 2011, 6(8), 845-856.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compounds Library Max Anti-Cancer Compound Library Ion Channel Inhibitor Library Potassium Channel Blocker Library NO PAINS Compound Library Bioactive Compound Library

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Keywords

ML133 hydrochloride 1222781-70-5 Membrane transporter/Ion channel Potassium Channel ML133 HCl KcsA Inhibitor inhibit ML 133 Hydrochloride ML-133 Hydrochloride ML 133 ML-133 hydrochloride ML133 ML133 Hydrochloride ML-133 inhibitor

 

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