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Merck

422689

Kir2.1 Inhibitor, ML133

The Kir2.1 Inhibitor, ML133, also referenced under CAS 185669-79-8, controls the biological activity of Kir2.1. This small molecule/inhibitor is primarily used for Cancer applications.

Synonym(s):

Kir2.1 Inhibitor, ML133, Inward rectifier potassium channel blocker, ML133

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About This Item

Empirical Formula (Hill Notation):
C19H19NO
CAS Number:
Molecular Weight:
277.36
UNSPSC Code:
12352200
NACRES:
NA.28
MDL number:

Product Name

Kir2.1 Inhibitor, ML133, The Kir2.1 Inhibitor, ML133, also referenced under CAS 185669-79-8, controls the biological activity of Kir2.1. This small molecule/inhibitor is primarily used for Cancer applications.

InChI

1S/C19H19NO/c1-21-18-11-9-15(10-12-18)13-20-14-17-7-4-6-16-5-2-3-8-19(16)17/h2-12,20H,13-14H2,1H3

SMILES string

COC(C=C1)=CC=C1CNCC2=C(C=CC=C3)C3=CC=C2

InChI key

GIFYKGIODMXYNT-UHFFFAOYSA-N

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 10 mg/mL, clear, colorless

shipped in

ambient

storage temp.

2-8°C

Quality Level

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable, renal outer medullary potassium (ROMK) blocker that is shown to inhibit inward rectifier potassium channel, Kir2.1 (IC50 = 1.8 µM and 290 nM, at pH 7.4 and pH 8.5, respectively). It exhibits little selectivity against other members of the Kir2.x family, but has no effect on Kir1.1 (IC50 >300 µM) and displays weak activity for Kir4.1 and Kir7.1 (IC50 = 76 µM and 33 µM, respectively). It is reported to be assayed in 218 MLPCN HTS campaigns, demonstrating activity in only two assays that are not based on Kir2.1. Furthermore, it displays a relatively clean profile in a radioligand binding panel of 68 GPCRs, ion channels and transporters.

Other Notes

Lindsley, C.W., et al. 2011. ACS Chem. Biol.6, 845.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Polarized localization of phosphatidylserine in the endothelium regulates Kir2.1.
Ruddiman, et al.
JCI insight, 8 (2023)

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