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ML133 hydrochloride

Cat. No. M2181
ML133 hydrochloride Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 77 In stock
25mg USD 177 In stock
50mg USD 250 In stock
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Quality Control
Biological Activity

ML133 hydrochloride is a potent K(ir)2.1 inhibitor, which inhibits K(ir)2.1 with an 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 hydrochloride has no effect on K(ir)1.1 (IC50 > 300 μM) and displays weak activity for K(ir)4.1 (76 μM) and K(ir)7.1 (33 μM). ML133 HCl also displays modest selectivity versus hERG and possesses fair ancillary pharmacology against a larger panel of GPCRs, ion channels and transporters.

Customer Product Validations & Biological Datas
Source Front Cell Neurosci (2015). Figure 3.ML133
Method CyQUANT proliferation assay
Cell Lines Microglial cells
Concentrations 20 μM
Incubation Time 24 h
Results Because both Kir2.1 blockers (Ba2+, ML133) greatly reduced migration, we asked whether their morphology changed to that of LPS-stimulated cells. It did not; and blocking Kir2.1 did not obviously affect their unipolar morphology under any of the activation states examined
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 313.82
Formula C19H19NO.HCl
CAS Number 1222781-70-5
Purity >99%
Solubility DMSO 43 mg/mL
Storage at -20°C

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.
Wang HR, et al. ACS Chem Biol. 2011 Aug 19;6(8):845-56. PMID: 21615117.

A potent and selective small molecule Kir2.1 inhibitor.
Wu M, et al. Probe Reports from the NIH Molecular Libraries Program [Internet]. 2010 Feb 26. PMID: 21433384.

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Abmole Inhibitor Catalog 2017

Keywords: ML133 hydrochloride supplier, Potassium Channel, inhibitors

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