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Merck

5.30923

Kir6.2/SUR1 Channel Activator, VU0071063

Synonym(s):

Kir6.2/SUR1 Channel Activator, VU0071063, 1,3-Dimethyl-7-(4-(2-methyl-2-propanyl)benzyl)-3,7-dihydro-1H-purine-2,6-dione, 7-(4-( tert-Butyl)benzyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione, Kir6.2/SUR1 Channel Opener, SUR1/Kir6.2 selective K-ATP Channel Opener, 1,3-Dimethyl-7-(4-(2-methyl-2-propanyl)benzyl)-3,7-dihydro-1H-purine-2,6-dione, 7-(4-(tert-Butyl)benzyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione, Kir6.2/SUR1 Channel Opener, SUR1/Kir6.2 selective K-ATP Channel Opener

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About This Item

Empirical Formula (Hill Notation):
C18H22N4O2
CAS Number:
333415-38-6
Molecular Weight:
326.39
MDL number:
MFCD02648040
UNSPSC Code:
12352200
NACRES:
NA.77

InChI key

ZFZAIHKQJBMYLO-UHFFFAOYSA-N

InChI

1S/C18H22N4O2/c1-18(2,3)13-8-6-12(7-9-13)10-22-11-19-15-14(22)16(23)21(5)17(24)20(15)4/h6-9,11H,10H2,1-5H3

SMILES string

[n]1(c2nc[n](c2[c]([n]([c]1=O)C)=O)Cc3ccc(cc3)C(C)(C)C)C

assay

≥97% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 100 mg/mL

storage temp.

2-8°C

Quality Level

100

Biochem/physiol Actions

EC50 = 7 µM for Kir6.2/SUR1 channel activation
Primary Target
SUR1-containing channels
Reversible: yes

Disclaimer

Toxicity: Standard Handling (A)

General description

A xanthine derivative that serves as a fast acting, reversible, and selective activator of Kir6.2/SUR1 channels (EC50 = 7 µM). Directly occupies the binding site located within SUR1. Shown to be a more potent activator of Kir6.2/SUR1 than diazoxide (EC50 = 120 µM). However, it does not affect Kir6.1/SURA2A or Kir6.2/SURA2A channels and is inactive against Kir2.1 and Kir2.2 (IC50 >100 µM) and exhibits very weak inhibitory activity against Kir3.1/3.2 (IC50 = 65 µM) and Kir2.3 (IC50 = 91 µM) channels. Inhibits glucose-stimulated Ca2+ influx into mouse pancreatic β-cells.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Other Notes

Raphemot, R., et al. 2014. Mol. Pharmacol.85, 858.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

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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